Comprehensive Survey of Combinatorial Library Synthesis: 2005

The Design of Leadlike Combinatorial Libraries

1999 • 765 citations

Is There a Difference between Leads and Drugs? A Historical Perspective

2001 • 757 citations

Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors

2004 • 494 citations

Discovery and Cocrystal Structure of Benzodiazepinedione HDM2 Antagonists That Activate p53 in Cells

2005 • 419 citations

Identification of a new antitubercular drug candidate, SQ109, from a combinatorial library of 1,2-ethylenediamines

2005 • 359 citations

Activity-based probes that target diverse cysteine protease families

2005 • 346 citations

In Situ Selection of Lead Compounds by Click Chemistry: Target-Guided Optimization of Acetylcholinesterase Inhibitors

2005 • 326 citations

Noble‐Metal Nanotubes (Pt, Pd, Ag) from Lyotropic Mixed‐Surfactant Liquid‐Crystal Templates

2003 • 269 citations

Comprehensive Survey of Combinatorial Library Synthesis: 2000

2001 • 259 citations

A New Principle in Combinatorial Asymmetric Transition‐Metal Catalysis: Mixtures of Chiral Monodentate P Ligands

2003 • 252 citations

Discovery of a Potent Small Molecule IL-2 Inhibitor through Fragment Assembly

2003 • 234 citations

Automated Library Generation Using Sequential Microwave-Assisted Chemistry. Application toward the Biginelli Multicomponent Condensation

2001 • 228 citations

Isolation of Protein Ligands from Large Peptoid Libraries

2003 • 212 citations

Discovery and Structure−Activity Relationship of Quinuclidine Benzamides as Agonists of α7 Nicotinic Acetylcholine Receptors

2005 • 207 citations

Synthesis and biological evaluation of benzothiazole derivatives as potent antitumor agents

2005 • 195 citations

One-pot synthesis of dihydropyrimidinones catalysed by lithium bromide: an improved procedure for the Biginelli reaction

2003 • 181 citations

Identification and Biological Evaluation of 4-(3-Trifluoromethylpyridin-2-yl)piperazine-1-carboxylic Acid (5-Trifluoromethylpyridin-2-yl)amide, a High Affinity TRPV1 (VR1) Vanilloid Receptor Antagonist

2004 • 179 citations

Global analysis of proteasomal substrate specificity using positional-scanning libraries of covalent inhibitors

2001 • 177 citations

Novel procedure for the synthesis of 1,3,4-oxadiazoles from 1,2-diacylhydrazines using polymer-supported Burgess reagent under microwave conditions

1999 • 176 citations

Phenol Ugi–Smiles Systems: Strategies for the Multicomponent N‐Arylation of Primary Amines with Isocyanides, Aldehydes, and Phenols

2005 • 169 citations

1,4-Benzodiazepine-2,5-diones as small molecule antagonists of the HDM2–p53 interaction: discovery and SAR

2004 • 163 citations

A novel three-component one-pot synthesis of pyrano[2,3-d]pyrimidines and pyrido[2,3-d]pyrimidines using microwave heating in the solid state

2003 • 162 citations

Discovery of Potent Chromen-4-one Inhibitors of the DNA-Dependent Protein Kinase (DNA-PK) Using a Small-Molecule Library Approach

2005 • 162 citations

The First Synthetic Application of a Monooxygenase Employing Indirect Electrochemical NADH Regeneration

2001 • 161 citations

Combinatorial Approach to Organelle-Targeted Fluorescent Library Based on the Styryl Scaffold

2003 • 153 citations

Beta-lactam compounds as apparently uncompetitive inhibitors of HIV-1 protease

2005 • 152 citations

Printing chemical libraries on microarrays for fluid phase nanoliter reactions

2003 • 146 citations

HR22C16: A Potent Small‐Molecule Probe for the Dynamics of Cell Division

2003 • 145 citations

Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines

2001 • 145 citations

Facilitated Forward Chemical Genetics Using a Tagged Triazine Library and Zebrafish Embryo Screening

2003 • 144 citations

Asymmetric Catalysis on Sequentially-Linked Columns

2001 • 144 citations

Synthesis of 7200 Small Molecules Based on a Substructural Analysis of the Histone Deacetylase Inhibitors Trichostatin and Trapoxin

2001 • 143 citations

Synthesis, Reaction, and Recycle of Light Fluorous Grubbs−Hoveyda Catalysts for Alkene Metathesis

2005 • 141 citations

Potent and Selective Aurora Inhibitors Identified by the Expansion of a Novel Scaffold for Protein Kinase Inhibition

2005 • 141 citations

Dynamic Deconvolution of a Pre-Equilibrated Dynamic Combinatorial Library of Acetylcholinesterase Inhibitors

2001 • 141 citations

Selective Inhibition of Factor Inhibiting Hypoxia-Inducible Factor

2005 • 140 citations

Hydrogenation and Dehalogenation under Aqueous Conditions with an Amphiphilic-Polymer-Supported Nanopalladium Catalyst

2004 • 140 citations

Oxidizing Polymers: A Polymer-Supported, Recyclable Hypervalent Iodine(V) Reagent for the Efficient Conversion of Alcohols, Carbonyl Compounds, and Unsaturated Carbamates in Solution J.R. gratefully acknowledges generous support from Prof. M. E. Maier, Tübingen, the Strukturfonds of the University of Tübingen, the Fonds der Chemischen Industrie, and the DFG. We thank Graeme Nicholson, Dietmar Schmid, and Daniel Bischoff for analytical support.

2001 • 137 citations

Cu(II)−Aza(bisoxazoline)-Catalyzed Asymmetric Benzoylations

2005 • 134 citations

A novel one-pot three-component reaction: Synthesis of triheterocyclic 4H-pyrimido[2,1-b]benzazoles ring systems

2005 • 131 citations

The Synthesis and Oxidative Properties of Polymer-Supported IBX

2001 • 129 citations

Di(2-pyridyl)methylamine–palladium dichloride complex covalently anchored to a styrene-maleic anhydride co-polymer as recoverable catalyst for C–C cross-coupling reactions in water

2005 • 127 citations

Influenza Neuraminidase Inhibitors: Structure-Based Design of a Novel Inhibitor Series

2003 • 123 citations

Identification of a Small Molecule Inhibitor of the IL-2/IL-2Rα Receptor Interaction Which Binds to IL-2

1997 • 123 citations

A Novel Highly Selective Chiral Auxiliary for the Asymmetric Synthesis of<scp>l</scp>- and<scp>d</scp>-α-Amino Acid Derivatives via a Multicomponent Ugi Reaction

2004 • 121 citations

Combinatorial Optimization of Isatin-β-Thiosemicarbazones as Anti-poxvirus Agents

2005 • 120 citations

Synthesis of 3,5-disubstituted-1,2,4-oxadiazoles using tetrabutylammonium fluoride as a mild and efficient catalyst

2001 • 117 citations

High-Throughput Synthesis of N3-Acylated Dihydropyrimidines Combining Microwave-Assisted Synthesis and Scavenging Techniques

2003 • 115 citations

Solvent-Free Asymmetric Olefin Hydroformylation Catalyzed by Highly Cross-Linked Polystyrene-Supported (R,S)-BINAPHOS−Rh(I) Complex

2003 • 115 citations

Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities

2005 • 114 citations

Microwave-assisted multi-component synthesis of fused 3-aminoimidazoles

2003 • 111 citations

Forward chemical genetics: progress and obstacles on the path to a new pharmacopoeia

2003 • 107 citations

The Recent Impact of Solid-Phase Synthesis on Medicinally Relevant Benzoannelated Oxygen Heterocycles

2005 • 107 citations

Incorporation of Unprotected Heterocyclic Side Chains into Peptoid Oligomers via Solid-Phase Submonomer Synthesis

2003 • 105 citations

The rapid preparation of 2-aminosulfonamide-1,3,4-oxadiazoles using polymer-supported reagents and microwave heating

2005 • 105 citations

Comprehensive Survey of Combinatorial Library Synthesis: 2004

2005 • 105 citations

An Alkylsilyl-Tethered, High-Capacity Solid Support Amenable to Diversity-Oriented Synthesis for One-Bead, One-Stock Solution Chemical Genetics

2001 • 104 citations

Rapid and diverse route to natural product-like biaryl ether containing macrocycles

2003 • 103 citations

Bisaryloxime Ethers as Potent Inhibitors of Transthyretin Amyloid Fibril Formation

2005 • 101 citations

Crystallization of an Ordered Mesoporous Nb–Ta Oxide

2003 • 100 citations

Ketones as Building Blocks for Dynamic Combinatorial Libraries: Highly Active Neuraminidase Inhibitors Generated via Selection Pressure of the Biological Target

2003 • 100 citations

2,6-Disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-Dependent protein kinase (DNA-PK)

2003 • 99 citations

Template-Mediated Synthesis of Polycyclic Aromatic Hydrocarbons: Cyclodehydrogenation and Planarization of a Hexaphenylbenzene Derivative at a Copper Surface

1999 • 99 citations

Solid-Phase Synthesis of a Nonpeptide RGD Mimetic Library: New Selective αvβ3 Integrin Antagonists

2001 • 98 citations

Spatially Resolved Detection of Neurotransmitter Secretion from Individual Cells by Means of Scanning Electrochemical Microscopy

2001 • 97 citations

Synthesis and Identification of Small Molecules that Potently Induce Apoptosis in Melanoma Cells through G1 Cell Cycle Arrest

2005 • 95 citations

Solid-Phase Synthesis of Indolecarboxylates Using Palladium-Catalyzed Reactions

2003 • 95 citations

Detection of Ligands from a Dynamic Combinatorial Library by X‐ray Crystallography

2003 • 94 citations

Radical Carbonylation/Reductive Cyclization for the Construction of Tetrahydrofuran-3-ones and Pyrrolidin-3-ones

2003 • 94 citations

The First Potent and Selective Inhibitors of the Glycine Transporter Type 2

2001 • 92 citations

Development of Small Molecule Hsp90 Inhibitors: Utilizing Both Forward and Reverse Chemical Genomics for Drug Identification

2003 • 92 citations

Trimethylsilyl-Directed 1,3-Dipolar Cycloaddition Reactions in the Solid-Phase Synthesis of 1,2,3-Triazoles

2005 • 91 citations

Asymmetric Allylsilane Additions to Enantiopure N-Acylhydrazones with Dual Activation by Fluoride and In(OTf)3 We thank the National Science Foundation (Vermont EPSCoR) and the University of Vermont for generous support.

2001 • 90 citations

Preparation of Thioamide Building Blocks via Microwave-Promoted Three-Component Kindler Reactions

2002 • 90 citations

Solution-phase synthesis of novel Δ2-isoxazoline libraries via 1,3-dipolar cycloaddition and their antifungal properties

2003 • 90 citations

Polymer-bound aluminium salen complex as reusable catalysts for CO2 insertion into epoxides

2005 • 90 citations

A Three‐Component Reaction for Diversity‐Oriented Synthesis of Polysubstituted Piperidines: Solution and Solid‐Phase Optimization of the First Tandem Aza[4+2]/Allylboration

2003 • 90 citations

Isoindolinone-based inhibitors of the MDM2–p53 protein–protein interaction

2005 • 89 citations

A Novel Three-Component Butenolide Synthesis

2001 • 87 citations

Expedient Synthesis and Design Strategies for New Peptoid Construction

2005 • 86 citations

Multipolymer Solution-Phase Reactions: Application to the Mitsunobu Reaction

2004 • 84 citations

Multiple Component Reactions: An Efficient Nickel-Catalyzed Reformatsky-Type Reaction and Its Application in the Parallel Synthesis of β-Amino Carbonyl Libraries

2003 • 84 citations

A Synthetic Library of Cell-Permeable Molecules

2000 • 83 citations

An Efficient Combination of Microwave Dielectric Heating and the Use of Solid-Supported Triphenylphosphine for Wittig Reactions

2001 • 82 citations

A three-component synthesis of pyrido[2,3-d]pyrimidines

2003 • 82 citations

Asymmetric Catalysis in Diversity-Oriented Organic Synthesis: Enantioselective Synthesis of 4320 Encoded and Spatially Segregated Dihydropyrancarboxamides

2001 • 81 citations

Parallel synthesis of 1,2,4-oxadiazoles from carboxylic acids using an improved, uronium-based, activation

2001 • 81 citations

Parallel Synthesis of a Vitamin D₃ Library in the Solid-Phase

2001 • 78 citations

Traceless solid phase synthesis of 2-substituted pyrimidines using an ‘off-the-shelf’ chlorogermane-functionalised resin

2003 • 78 citations

Solid-Phase Synthesis of Oligourea Peptidomimetics Employing the Fmoc Protection Strategy

2001 • 78 citations

Discovery of Estrogen Sulfotransferase Inhibitors from a Purine Library Screen

2001 • 76 citations

Solid-Phase Total Synthesis of the Pentacyclic System Lamellarins U and L

2003 • 76 citations

Parallel synthesis of 1,2,4-oxadiazoles using CDI activation

1999 • 76 citations

Parallel synthesis and biological evaluation of 5,6,7,8-tetrahydrobenzothieno[2,3-d]pyrimidin-4(3H)-one cytotoxic agents selective for p21-deficient cells

2005 • 76 citations

Identification from a Combinatorial Library of a Small Molecule that Selectively Induces Apoptosis in Cancer Cells

2003 • 74 citations

Solid-Phase Synthesis of Urea and Amide Libraries Using the T2 Triazene Linker

2000 • 74 citations

A Metal–Carbene Carbohydrate Amphiphile as a Low‐Molecular‐Mass Organometallic Gelator

2003 • 74 citations

Traceless Solid-Phase Synthesis of Substituted Benzimidazoles via a Base-Cleavable Linker

2000 • 73 citations

Synthesis and SAR of cis-1-Benzoyl-1,2,3,4-tetrahydroquinoline ligands for control of gene expression in ecdysone responsive systems

2003 • 73 citations

Novel Polymer-Bound Chiral Selenium Electrophiles

2001 • 72 citations

Stereocontrolled Solid‐Phase Synthesis of a 90‐Membered Library of Indoline‐Alkaloid‐like Polycycles from an Enantioenriched Aminoindoline Scaffold

2005 • 72 citations

Cross-metathesis reaction. Generation of highly functionalized olefins from unsaturated alcohols

2001 • 72 citations

Polymer-Supported Pyridine−Bis(oxazoline). Application to Ytterbium-Catalyzed Silylcyanation of Benzaldehyde

2003 • 72 citations

Identification of small molecule inhibitors of the hepatitis C virus RNA-dependent RNA polymerase from a pyrrolidine combinatorial mixture

2005 • 70 citations

Chromium(<scp>V</scp>) and Chromium(<scp>VI</scp>) Nitrido Complexes of Tris(pentafluorophenyl)corrole

2003 • 70 citations

Cellulose Beads: a New Versatile Solid Support for Microwave- Assisted Synthesis. Preparation of Pyrazole and Isoxazole Libraries

2003 • 70 citations

Ligand-Based Combinatorial Design of Selective Purinergic Receptor (A_2A) Antagonists Using Self-Organizing Maps

2003 • 70 citations

Solution-phase parallel synthesis of 4,6-diaryl-pyrimidine-2-ylamines and 2-amino-5,5-disubstituted-3,5-dihydro-imidazol-4-ones via a rearrangement

2003 • 69 citations

2,5-Diketopiperazines as potent and selective oxytocin antagonists 1: identification, stereochemistry and initial SAR

2005 • 69 citations

2-Aryl Indole NK1 receptor antagonists: optimisation of indole substitution

2001 • 69 citations

A Fluorous‐Phase Pummerer Cyclative‐Capture Strategy for the Synthesis of Nitrogen Heterocycles

2004 • 69 citations

Solution and Solid-Supported Synthesis of 3,4,5-Trisubstituted 1,2,4-Triazole-Based Peptidomimetics

2003 • 68 citations

Synthesis of functionalized heterocycles via a tandem Staudinger/aza-Wittig/Ugi multicomponent reaction

2005 • 67 citations

Expanding the diversity of purine libraries

2001 • 67 citations

Design, Synthesis, and Utility of a Support-Bound tert-Butanesulfinamide

2001 • 66 citations

DNA Binding Ligands Targeting Drug-Resistant Bacteria: Structure, Activity, and Pharmacology

2003 • 66 citations

Discovery of a novel CCR3 selective antagonist

2001 • 66 citations

Dihydropyridine-Based Multicomponent Reactions. Efficient Entry into New Tetrahydroquinoline Systems through Lewis Acid-Catalyzed Formal [4 + 2] Cycloadditions

2003 • 66 citations

Split−Pool Synthesis of 1,3-Dioxanes Leading to Arrayed Stock Solutions of Single Compounds Sufficient for Multiple Phenotypic and Protein-Binding Assays

2001 • 65 citations

Development of Natural Product-Derived Receptor Tyrosine Kinase Inhibitors Based on Conservation of Protein Domain Fold

2003 • 65 citations

Practical Synthesis of Unsymmetrical Ureas from Isopropenyl Carbamates

2005 • 64 citations

Solid-Phase Synthesis of 1,2,3-Triazoles via 1,3-Dipolar Cycloaddition

2003 • 64 citations

Diastereoselective Solution and Multipin‐Based Combinatorial Array Synthesis of a Novel Class of Potent Phosphinic Metalloprotease Inhibitors

2003 • 63 citations

Cycloisomerization of 1,6-Enynes: Asymmetric Multistep Preparation of a Hydrindane Framework in Water with Polymeric Catalysts

2004 • 63 citations

A Combinatorial Approach to [1,5]Benzothiazepine Derivatives as Potential Antibacterial Agents

2001 • 63 citations

Pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides as novel anti-proliferative agents: parallel synthesis for lead optimization of amide region

2005 • 62 citations

Identification, Synthesis, and Activity of Novel Blockers of the Voltage-Gated Potassium Channel Kv1.5

2003 • 62 citations

Discovery of Tyrosine-Based Potent and Selective Melanocortin-1 Receptor Small-Molecule Agonists with Anti-inflammatory Properties

2003 • 62 citations

Parallel Synthesis and Biological Screening of Dopamine Receptor Ligands Taking Advantage of a Click Chemistry Based BAL Linker

2005 • 62 citations

Amino-Functionalized Ionic Liquid as A Nucleophilic Scavenger in Solution Phase Combinatorial Synthesis

2005 • 61 citations

Inhibitors ofTrypanosoma cruziTrypanothione Reductase Revealed by Virtual Screening and Parallel Synthesis

2005 • 60 citations

Linked Parallel Synthesis and MTT Bioassay Screening of Substituted Chalcones

2001 • 60 citations

Generation of Bis-Cationic Heterocyclic Inhibitors of Bacillus subtilis HPr Kinase/Phosphatase from a Ditopic Dynamic Combinatorial Library

2003 • 60 citations

Bartoli Indole Synthesis on Solid Supports

2003 • 60 citations

Solid-Phase Rhodium Carbenoid Reactions: An N−H Insertion Route to a Diverse Series of Oxazoles

2001 • 60 citations

A Nanoscopic Molecular Cadmium Phosphonate Wrapped in a Hydrocarbon Sheath

2003 • 59 citations

The discovery of sulfonylated dipeptides as Potent VLA-4 antagonists

2001 • 59 citations

Synthesis of oxadiazoles on solid support

1999 • 59 citations

Solid-Phase Synthesis of Pyrroloisoquinolines via the Intramolecular N-Acyliminium Pictet−Spengler Reaction

2005 • 59 citations

Performing the Synthesis of a Complex Molecule on Sequentially Linked Columns: Toward the Development of a “Synthesis Machine”

2005 • 59 citations

Small-Molecule Diversity Using a Skeletal Transformation Strategy

2005 • 59 citations

Biphenylsulfonamide Endothelin Receptor Antagonists. 4. Discovery of N-[[2‘-[[(4,5-Dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1‘-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), A Highly Potent and Orally Active ET_A Selective Antagonist

2002 • 59 citations

Statistical Molecular Design, Parallel Synthesis, and Biological Evaluation of a Library of Thrombin Inhibitors

2001 • 59 citations

Versatile strategies for the solid phase synthesis of small heterocyclic scaffolds: [1,3,4]-thiadiazoles and [1,3,4]-oxadiazoles

2005 • 59 citations

Synthesis of tetrasubstituted thiophenes on solid-support using the Gewald reaction

2001 • 58 citations

Synthesis and Biological Evaluation of an Indomethacin Library Reveals a New Class of Angiogenesis‐Related Kinase Inhibitors

2003 • 58 citations

Design of Small-Sized Libraries by Combinatorial Assembly of Linkers and Functional Groups to a Given Scaffold: Application to the Structure-Based Optimization of a Phosphodiesterase 4 Inhibitor

2005 • 58 citations

Novel and Potent 17β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors

2005 • 58 citations

Sulfide- and selenide-based linkers in phase tag-assisted synthesis

2005 • 57 citations

Lewis Acid Catalyzed Solid-Phase Synthesis of Flavonoids Using Selenium-Bound Resin

2005 • 56 citations

Combinatorial modification of natural products: synthesis and in vitro analysis of derivatives of thiazole peptide antibiotic GE2270 A: A-ring modifications

2003 • 56 citations

Solid-phase synthesis of benzimidazole libraries biased for RNA targets

2003 • 56 citations

Untitled

1998 • 55 citations

Preparation of Unsymmetrical Sulfonylureas from N,N‘-Sulfuryldiimidazoles

2002 • 55 citations

Solid-Phase Synthesis of Bleomycin Group Antibiotics. Construction of a 108-Member Deglycobleomycin Library

2003 • 55 citations

Synthesis and SAR of novel 4,5-diarylimidazolines as potent P2X7 receptor antagonists

2004 • 55 citations

A novel, base-labile fluorous amine protecting group: synthesis and use as a tag in the purification of synthetic peptides

2003 • 54 citations

Solid-Phase Synthesis of β-Lactams via the Miller Hydroxamate Approach

2001 • 54 citations

Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists

2003 • 54 citations

A Mild and General Solid-Phase Method for the Synthesis of Chiral Polyamines. Solution Studies on the Cleavage of Borane−Amine Intermediates from the Reduction of Secondary Amides

2001 • 54 citations

MCC/SNAr methodology. Part 2: Novel three-step solution phase access to libraries of benzodiazepines

2003 • 53 citations

Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56Lck

2003 • 53 citations

2-Hydroxy-4,6-diamino-[1,3,5]triazines: A Novel Class of VEGF-R2 (KDR) Tyrosine Kinase Inhibitors

2004 • 52 citations

Solid-Phase Synthesis of Conformationally Constrained Peptidomimetics Based on a 3,6-Disubstituted-1,4-diazepan-2,5-dione Core

2003 • 52 citations

Recent advances in 1,3-dipolar cycloaddition reactions on solid supports

2005 • 52 citations

Conformationally Constrained 1,3-Diamino Ketones: A Series of Potent Inhibitors of the Cysteine Protease Cathepsin K

1998 • 52 citations

Quinazolinethiones and quinazolinediones, novel inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure–activity relationships

2004 • 51 citations

Design of Selective Peptidomimetic Agonists for the Human Orphan Receptor BRS-3

2003 • 51 citations

Solid-phase synthesis of pyrrolo[2,1- c ] [1,4] benzodiazepine-5,11-diones

2001 • 50 citations

A Novel Traceless Solid-Phase Friedländer Synthesis

2003 • 50 citations

An expedient synthesis of 3-acyltetramic acids of the melophlin family from α-aminoesters and immobilized Ph3PCCO

2005 • 50 citations

Solid-phase synthesis of cyclic RGD-furanoid sugar amino acid peptides as integrin inhibitors

2003 • 50 citations

Combinatorial library of five-membered iminocyclitol and the inhibitory activities against glyco-enzymes

2001 • 50 citations

Parallel Solution-Phase Asymmetric Synthesis of α-Branched Amines

2003 • 50 citations

Synthesis and Reactions of Fluorous Carbobenzyloxy (^FCbz) Derivatives of α-Amino Acids

2003 • 49 citations

Synthesis and biological evaluation of deoxypreussomerin A and palmarumycin CP1 and related naphthoquinone spiroketals

2001 • 49 citations

1,4-Diazepane-2-ones as novel inhibitors of LFA-1

2003 • 49 citations

Fluorous Dienophiles Are Powerful Diene Scavengers in Diels−Alder Reactions

2003 • 49 citations

Solid-Phase Synthesis and Inhibitory Effects of Some Pyrido[1,2-c]pyrimidine Derivatives on Leukocyte Functions and Experimental Inflammation

2001 • 48 citations

Synthesis of Solution-Phase Combinatorial Library of 4,6-Diamino-1,2-dihydro-1,3,5-triazine and Identification of New Leads Against A16V+S108T Mutant Dihydrofolate Reductase of Plasmodium falciparum

2003 • 48 citations

A Positional Scanning Combinatorial Library of Peptoids As a Source of Biological Active Molecules: Identification of Antimicrobials

2003 • 48 citations

MeOPEG-bounded azide cycloadditions to alkynyl dipolarophiles

2003 • 48 citations

Traceless solid-phase synthesis of 2-amino-5-alkylidene-thiazol-4-ones

2005 • 48 citations

Trifluoroacetic Anhydride-Mediated Solid-Phase Version of the Robinson−Gabriel Synthesis of Oxazoles

2005 • 48 citations

Hyperstranded DNA Architectures Observed by Cold‐Spray Ionization Mass Spectrometry

2003 • 47 citations

Discovery of a New Phosphotyrosine Mimetic for PTP1B Using Breakaway Tethering

2003 • 47 citations

Design, synthesis and preliminary biological evaluation of a focused combinatorial library of stereodiverse carbohydrate-scaffold-based peptidomimetics

2001 • 47 citations

Multicomponent Reactions with Dihydroazines: Efficient Synthesis of a Diverse Set of Pyrido-Fused Tetrahydroquinolines

2004 • 47 citations

The First Solid-Phase Synthesis of Bis(oxazolinyl)pyridine Ligands

2005 • 47 citations

Hydrophilic Polymer Supports for Solid-Phase Synthesis: Preparation of Poly(ethylene glycol) Methacrylate Polymer Beads Using “Classical” Suspension Polymerization in Aqueous Medium and Their Application in the Solid-Phase Synthesis of Hydantoins

2001 • 46 citations

Quinic Acid Derivatives as Sialyl Lewis^x-Mimicking Selectin Inhibitors: Design, Synthesis, and Crystal Structure in Complex with E-Selectin

2005 • 46 citations

Polymer-supported chiral sulfonamide catalyzed one-pot reduction of β-keto nitriles: a practical synthesis of (R)-fluoxetine and (R)-duloxetine

2005 • 46 citations

Microwave-initiated living free radical polymerization: rapid formation of custom Rasta resins

2003 • 45 citations

Traceless Solid-Phase Synthesis of 1,2,4-Triazoles Using a Novel Amine Resin

2001 • 45 citations

N- and C-terminal modifications of negamycin

2003 • 45 citations

(Cyanomethyl)trialkylphosphonium Iodides: Efficient Reagents for the Intermolecular Alkylation of Amines with Alcohols in Solution and on Solid Phase

2001 • 44 citations

Structure-Based Design, Parallel Synthesis, Structure−Activity Relationship, and Molecular Modeling Studies of Thiocarbamates, New Potent Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitor Isosteres of Phenethylthiazolylthiourea Derivatives

2005 • 44 citations

Repetitive Ugi reactions

2001 • 44 citations

Solid-phase synthesis of substituted 1,3,4-thiadiazoles

2003 • 44 citations

A new method for the synthesis of plurisubstituted pyrroles

2003 • 44 citations

Short and Novel Stereospecific Synthesis of Trisubstituted 2,5-Diketopiperazines

2005 • 43 citations

Liquid-Phase Synthesis of Combinatorial Libraries Based on 7-Trifluoromethyl-Substituted Pyrazolo[1,5-a]Pyrimidine Scaffold

2005 • 43 citations

Solid Phase Synthesis of Pyridine-Based Derivatives from a 2-Chloro-5-Bromopyridine Scaffold

2005 • 43 citations

Microwave-assisted synthesis of 4,4′-diaminotriphenylmethanes

2005 • 43 citations

Tartric Acid-Based Linker for the Solid-Phase Synthesis of C-Terminal Peptide α-Oxo Aldehydes

2001 • 43 citations

Design and synthesis of new bicyclic diketopiperazines as scaffolds for receptor probes of structurally diverse functionality

2005 • 43 citations

Rapid Parallel Synthesis of Dipeptide Diphenyl Phosphonate Esters as Inhibitors of Dipeptidyl Peptidases

2003 • 43 citations

Synthesis and Biological activity of kappa opioid receptor agonists. Part 2: Preparation of 3-aryl-2-pyridone analogues generated by solution- and solid-phase parallel synthesis methods

2003 • 43 citations

Merrifield Resin-Supported Chain Transfer Agents, Precursors for RAFT Polymerization

2005 • 43 citations

2-(2-Oxo-1,4-dihydro-2H-quinazolin-3-yl)- and 2-(2,2-Dioxo-1,4-dihydro-2H-2λ⁶-benzo[1,2,6]thiadiazin-3-yl)-N-hydroxy-acetamides as Potent and Selective Peptide Deformylase Inhibitors

2001 • 42 citations

Thermal and microwave-assisted N-formylation using solid-supported reagents

2004 • 42 citations

Identification of Alkylidene Hydrazides as Glucagon Receptor Antagonists

2001 • 42 citations

A Phosphorane as Supported Acylanion Equivalent: Linker Reagents for Smooth and Versatile CC Coupling Reactions

2003 • 42 citations

Synthesis and pharmacological characterisation of 2,4-Dicarboxy-pyrroles as selective non-Competitive mGluR1 antagonists

2003 • 42 citations

1,3,4-Oxadiazole formation; a novel solid support strategy

2001 • 42 citations

Solid-Supported Cyclohexane-1,3-dione (CHD): A “Capture and Release” Reagent for the Synthesis of Amides and Novel Scavenger Resin

2003 • 42 citations

Parallel Synthesis of Glycomimetic Libraries: Targeting a C-Type Lectin

2003 • 41 citations

Combination of microwave reactions with fluorous separations in the palladium-catalyzed synthesis of aryl sulfides

2003 • 41 citations

3-(2-Benzyloxyphenyl)isoxazoles and isoxazolines: synthesis and evaluation as CFTR activators

2003 • 41 citations

Solid-Phase Synthesis of Diaryl Sulfides: Direct Coupling of Solid-Supported Aryl Halides with Thiols Using an Insoluble Polymer-Supported Reagent

2005 • 41 citations

Automated Parallel Solid-Phase Synthesis and Anticancer Screening of a Library of Peptide-Tethered Platinum(II) Complexes

2003 • 41 citations

A facile synthesis of 1,4-benzodiazepine derivatives via Ugi four-component condensation

2004 • 41 citations

Boronate Titanium Alkylidene Reagents for Diversity-Based Synthesis of Benzofurans

2003 • 41 citations

A rapid microwave-assisted esterification utilizing the Mukaiyama supported reagent

2005 • 41 citations

The Aminopalladation-Reductive Elimination Process as a Tool for the Solution-Phase Synthesis of 2,3-Disubstituted Azaindole Libraries

2005 • 40 citations

Design and synthesis of an optimized positional scanning library of peptoids: identification of novel multidrug resistance reversal agents

2005 • 40 citations

Solid-phase synthesis of asymmetric cyanine dyes

2001 • 39 citations

Solid-Phase Parallel Synthesis of 17α-Substituted Estradiol Sulfamate and Phenol Libraries Using the Multidetachable Sulfamate Linker

2003 • 39 citations

Structure-Based Development of Pyridoxal Propionate Derivatives as Specific Inhibitors of Cathepsin K in Vitro and in Vivo

2000 • 39 citations

Revolutionizing Resin Handling for Combinatorial Synthesis

2001 • 39 citations

Phenethyl Amides as Novel Noncovalent Inhibitors of Hepatitis C Virus NS3/4A Protease: Discovery, Initial SAR, and Molecular Modeling

2002 • 39 citations

Research on anti-HIV-1 agents. Part 2: Solid-phase synthesis, biological evaluation and molecular modeling studies of 2,5,6-trisubstituted-4(3H)-pyrimidinones targeting HIV-1 reverse transcriptase

2001 • 39 citations

Effect of spacers on the activity of soluble polymer supported catalysts for the asymmetric addition of diethylzinc to aldehydes

2003 • 39 citations

Solid-phase synthesis of imidazo[1,2-a]pyridines and imidazo[1,2-a]pyrimidines

2003 • 39 citations

Combinatorial synthesis of CCR5 antagonists

2001 • 38 citations

Inhibitors of hepatitis C virus NS3·4A protease 1. Non-Charged tetrapeptide variants

2003 • 38 citations

Novel and potent NPY5 receptor antagonists derived from virtual screening and iterative parallel chemistry design

2005 • 38 citations

Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry

2005 • 38 citations

An Exploratory Study on Microwave-Assisted Solid-Phase Diels−Alder Reactions of 2(1H)-Pyrazinones: the Elaboration of a New Tailor-Made Acid-Labile Linker

2003 • 38 citations

Fluorous chiral bisoxazolines. Synthesis and applications to an asymmetric allylic alkylation

2003 • 37 citations

Synthesis of a diverse set of phosphorus ligands on solid support and their screening in the Heck reaction

2003 • 37 citations

The Reversed Kenner Linker: A New Safety-Catch Linker for the Preparation of N-Alkyl Sulfonamides

2001 • 37 citations

Modulation of MRP-1-Mediated Multidrug Resistance by Indomethacin Analogues

2005 • 37 citations

pH-Dependent Changes in Photoaffinity Labeling Patterns of the H1 Influenza Virus Hemagglutinin by Using an Inhibitor of Viral Fusion

1999 • 36 citations

Preparation of a Fully Substituted Purine Library

2005 • 36 citations

The Development and Application of a Novel Safety-Catch Linker for BOC-Based Assembly of Libraries of Cyclic Peptides^,1

2001 • 36 citations

Solid-Phase Synthesis of Nucleoside Analogues

2003 • 36 citations

Use of MCSS to Design Small Targeted Libraries: Application to Picornavirus Ligands

2001 • 36 citations

Polystyrene-Supported (R)-2-Piperazino-1,1,2-triphenylethanol: A Readily Available Supported Ligand with Unparalleled Catalytic Activity and Enantioselectivity

2004 • 36 citations

Modular, Parallel Synthesis of an Illudinoid Combinatorial Library

2003 • 36 citations

Solid-Phase Synthesis of Peptide Esters Employing the Hydrazide Linker

2003 • 35 citations

Array synthesis of novel lipodepsipeptide

2003 • 35 citations

A Highly Efficient, Asymmetric Synthesis of Benzothiadiazine-Substituted Tetramic Acids: Potent Inhibitors of Hepatitis C Virus RNA-Dependent RNA Polymerase

2005 • 35 citations

Design and synthesis of a new polymer-supported Evans-type oxazolidinone: an efficient chiral auxiliary in the solid-phase asymmetric alkylation reactions

2005 • 35 citations

Design and pharmacology of peptoids and peptide–peptoid hybrids based on the melanocortin agonists core tetrapeptide sequence

2003 • 35 citations

Solid-Phase Synthesis of α,α-Difluoro-β-amino Acids via the Reformatsky Reaction

2001 • 35 citations

A new general three component solution-phase synthesis of 2-amino-1,3-thiazole and 2,4-diamino-1,3-thiazole combinatorial libraries

2001 • 35 citations

Creating chemical diversity space by scaffold decoration of dihydropyrimidines

2005 • 35 citations

Polymer-supported chiral phosphinooxathiane ligands for palladium-catalyzed asymmetric allylations

2005 • 34 citations

1,3-Dipolar cycloadditions of MeOPEG-bounded azides

2005 • 34 citations

High-throughput synthesis and optimization of thrombin inhibitors via urazole α-addition and Michael addition

2003 • 34 citations

Solution-Phase Synthesis of a Library of 3,5,7-Trisubstituted 3H-[1,2,3]triazolo[4,5-d]pyrimidines

2003 • 34 citations

Combinatorial Library of Peptide Isosters Based on Diels−Alder Reactions: Identification of Novel Inhibitors against a Recombinant Cysteine Protease fromLeishmania mexicana

2001 • 34 citations

Phenylpyrroles, a new chemolibrary virtual screening class of 5-HT7 receptor ligands

2005 • 34 citations

Novel semicarbazide-derived inhibitors of human dipeptidyl peptidase I (hDPPI)

2005 • 34 citations

General combinatorial synthesis of tertiary amines on solid support. A novel conditional release strategy based on traceless linking at nitrogen

2001 • 34 citations

Surfing the piperazine core of tricyclic farnesyltransferase inhibitors

2005 • 33 citations

Carbon–carbon bond construction on solid support: triethylborane-induced radical reactions of oxime ethers

2003 • 33 citations

Diversity Oriented Synthesis of Tricyclic Compounds from Glycals Using the Ferrier and the Pauson−Khand Reactions

2005 • 33 citations

The Bohlmann–Rahtz route to functionalised pyridine scaffolds and their use in library synthesis

2003 • 33 citations

Discovery of non-steroidal mifepristone mimetics: Pyrazoline-based PR antagonists

2005 • 33 citations

Direct Mono-N-methylation of Solid-Supported Amino Acids: A Useful Application of the Matteson Rearrangement of α-Aminoalkylboronic Esters

2001 • 33 citations

A Facile Solid-Phase Synthesis of Substituted 2(5H)-Furanones from Polymer-Supported α-Selenocarboxylic Acids

2003 • 33 citations

Selective and orally bioavailable phenylglycine tissue factor/factor VIIa inhibitors

2005 • 33 citations

Identification of a potent and selective oxytocin antagonist, from screening a fully encoded differential release combinatorial chemical library

2001 • 33 citations

A Library Approach to the Generation of Bisubstrate Analogue Sulfotransferase Inhibitors

2001 • 32 citations

2-Aryl-5,5-bisoxazolin-2-yl[1,3]dioxanes as solution phase and immobilised ligands for highly enantioselective cyclopropanations

2005 • 32 citations

Solid-phase Friedel–Crafts acylation on polystyrene resins-synthesis of antiepiletic 1-aryl-3,5-dihydro-4 H -2,3-benzodiazepin-4-ones

2001 • 31 citations

Polymer-Supported O-Benzyl and O-Allylisoureas: Convenient Preparation and Use in Ester Synthesis from Carboxylic Acids

2003 • 31 citations

Size Doesn't Matter: Scaffold Diversity, Shape Diversity and Biological Activity of Combinatorial Libraries

2003 • 31 citations

Multistep Parallel Synthesis of Quinazoline‐2,4‐diones by a Fluorous Biphasic Concept without Perfluorinated Solvents

2003 • 31 citations

An Acid-Stabletert-Butyldiarylsilyl (TBDAS) Linker for Solid-Phase Organic Synthesis

2005 • 31 citations

Solution- and Solid-Phase Parallel Synthesis of 4-Alkoxy-Substituted Pyrimidines with High Molecular Diversity

2003 • 31 citations

Novel solid-phase preparation of 2,6,9-trisubstituted purines for combinatorial library generation

2001 • 30 citations

Solid-phase syntheses of constrained RGD scaffolds and their binding to the αvβ3 integrin receptor

2001 • 30 citations

Solid phase β-lactams synthesis using the Staudinger reaction, monitored by 19F NMR spectroscopy

2003 • 30 citations

Versatile Solid-Phase Synthesis of Peptide-Derived 2-Oxazolines. Application in the Synthesis of Ligands for Asymmetric Catalysis

2005 • 30 citations

Solid-phase synthesis and solution structure of bicyclic β-turn peptidomimetics: diversity at the i position

2001 • 30 citations

Efficient reduction of aromatic nitro/azido groups on solid support employing indium: synthesis of pyrrolo[2,1-c][1,4]benzodiazepine-5,11-diones

2001 • 30 citations

Solid-Phase Mannich Condensation of Amines, Aldehydes, and Alkynes: Investigation of Diverse Aldehyde Inputs

2001 • 30 citations

An approach to the identification of potent inhibitors of influenza virus fusion using parallel synthesis methodology

2001 • 30 citations

Synthesis and Evaluation of 3-Methyl-4-oxo-6-phenyl-4,5,6,7-tetrahydrobenzofuran-2-carboxylic Acid Ethyl Ester Derivatives as Potent Antitumor Agents

2005 • 30 citations

Expedient Parallel Synthesis of 2-Amino-4-heteroarylpyrimidines

2005 • 30 citations

Alternative Solvents for Elevated-Temperature Solid-Phase Parallel Synthesis. Application to Thionation of Amides

2003 • 30 citations

Photochemical Generation of Nitrosocarbonyl Intermediates on Solid Phase: Synthons toward Hetero Diels−Alder and Ene Adducts through Photocleavage

2005 • 30 citations

The Effects of Conformational Constraints and Steric Bulk in the Amino Acid Moiety of Philanthotoxins on AMPAR Antagonism

2004 • 30 citations

Oxidosqualene Cyclase Inhibitors as Antimicrobial Agents

2003 • 30 citations

Facile Synthesis of a Library of 9-Alkyl-8-benzyl-9H-purin-6-ylamine Derivatives

2001 • 30 citations

Formation of 4-Aminopyrimidines via the Trimerization of Nitriles Using Focused Microwave Heating

2005 • 29 citations

Evolutionary Chemistry Approach toward Finding Novel Inhibitors of the Type 2 Diabetes Target Glucose-6-phosphate Translocase

2005 • 29 citations

Synthesis of novel exocyclic amino nucleosides by parallel solid-phase combinatorial strategy

2003 • 29 citations

Strategies for the synthesis of novel indole alkaloid-based screening libraries for drug discovery

2005 • 28 citations

A Combinatorial Scaffold Approach Based upon a Multicomponent Reaction

2003 • 28 citations

Generating Diversity in Difluoromethyl Ketone Derivatives

2001 • 28 citations

Minor structural modifications convert a selective PPARα agonist into a potent, highly selective PPARδ agonist

2005 • 28 citations

A Facile Solution Phase Combinatorial Synthesis of Tetrasubstituted Pyridines Using the Bohlmann-Rahtz Heteroannulation Reaction

2002 • 28 citations

Discovery of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid diamides that increase CFTR mediated chloride transport

2005 • 28 citations

Antibacterial activity of quinolone–Macrocycle conjugates

2003 • 28 citations

Synthesis and Evaluation of 17α-20E-21-(4-Substituted phenyl)-19-norpregna-1,3,5(10),20-tetraene-3,17β-diols as Probes for the Estrogen Receptor α Hormone Binding Domain

2003 • 28 citations

Solution-phase Synthesis of a Combinatorial Library of 3-[4-(Coumarin-3-yl)-1,3-thiazol-2-ylcarbamoyl]propanoic acid Amides

2005 • 27 citations

Efficient Synthesis and Environmentally Friendly Reactions of PEG-Supported 1,2-Diaza-1,3-butadiene

2005 • 27 citations

Solid-Phase Synthesis of Macrolide Analogues

2001 • 27 citations

A General Solid Phase Method for the Preparation of Diverse Azapeptide Probes Directed Against Cysteine Proteases

2005 • 27 citations

Asymmetric Mukaiyama aldol reaction of silyl enol ethers with aldehydes using a polymer-supported chiral Lewis acid catalyst

2005 • 27 citations

Solid-Phase Synthesis of Lidocaine and Procainamide Analogues Using Backbone Amide Linker (BAL) Anchoring

2003 • 27 citations

Fluorous click chemistry as a practical tagging method

2005 • 27 citations

Polystyrene-supported amino alcohol ligands for the heterogeneous asymmetric addition of phenyl zinc reagents to aldehydes

2005 • 27 citations

Efficient Solution Phase Combinatorial Access to a Library of Pyrazole- and Triazole-Containing Compounds

2003 • 27 citations

Anomeric activation of thioglycosides and preparation of deoxyglycosides using polymer-bound iodate(I) complexes

2003 • 27 citations

Parallel Synthesis of Antimalarial Rhodacyanine Dyes by the Combination of Three Components in One Pot

2003 • 27 citations

Radical Cyclization of 1,6-Diene Using Polystyrene-Supported Selenosulfones

2003 • 27 citations

Fluorous Mixture Synthesis of Fused-Tricyclic Hydantoins. Use of a Redundant Tagging Strategy on Fluorinated Substrates

2005 • 27 citations

Reusable resin plug-bound palladium catalysts for organic synthesis

2003 • 27 citations

Synthesis and biological evaluation of unnatural canthine alkaloids

2005 • 27 citations

Synthesis of 3-Amino-1,2,4-benzothiadi- azine 1,1-Dioxides via a Tandem Aza-Wittig/Heterocumulene Annulation

2005 • 26 citations

Reactivity of α-(Benzoyloxy)crotylstannane with Aldehydes in Liquid Phase and on Solid Support. Synthesis of Substituted Lactones

2001 • 26 citations

The facile preparation of primary and secondary amines via an improved Fukuyama–Mitsunobu procedure. Application to the synthesis of a lung-targeted gene delivery agent

2005 • 26 citations

Solid phase cross-coupling reaction of aryl(halo)silanes with 4-iodobenzoic acid

2001 • 26 citations

New Potential Antihistaminic Compounds. Virtual Combinatorial Chemistry, Computational Screening, Real Synthesis, and Pharmacological Evaluation

2005 • 26 citations

Fully automated multi-step solution phase synthesis using polymer supported reagents: preparation of histone deacetylase inhibitors

2003 • 26 citations

Solid/Solution‐Phase Annulation Reagents: Single‐Step Synthesis of Cyclic Amine Derivatives

2005 • 26 citations

Solid-Phase Synthesis of Libraries Generated from a 4-Phenyl-2-carboxy-piperazine Scaffold

2001 • 26 citations

Synthesis of a Sulfahydantoin Library

2001 • 26 citations

Solid-phase synthesis of oxygen-bridged tetrahydropyridones

2001 • 26 citations

Evaluation of a new linker system cleaved using samarium(ii) iodide. Application in the solid phase synthesis of carbonyl compounds

2005 • 26 citations

An Optimized Protein Kinase C Activating Diacylglycerol Combining High Binding Affinity (K_i) with Reduced Lipophilicity (log P)

2001 • 26 citations

A new approach in the solid-phase synthesis of polyamine derivatives: construction of polyamine backbones from the center

2001 • 26 citations

trans -3,4-Dimethyl-4-(3-carboxamidophenyl)piperidines: A novel class of μ-Selective opioid antagonists

2003 • 26 citations

A Straightforward, One-Pot Protocol for the Preparation of Libraries of 2-Oxazolines

2005 • 26 citations

Fluorous Mixture Synthesis of 4-Alkylidene Cyclopentenones via a Rhodium-Catalyzed [2+2+1] Cycloaddition of Alkynyl Allenes

2004 • 26 citations

Prodrugs to enhance central nervous system effects of the TRH-like peptide pGlu-Glu-Pro-NH2

2003 • 26 citations

Structure–activity relationship on the human EP3 prostanoid receptor by use of solid-support chemistry

2001 • 26 citations

A cyclative cleavage approach to solid-phase synthesis of annulated pyrimidinones using Baylis–Hillman derivatives

2005 • 25 citations

High Throughput Physical Organic Chemistry: Analytical Constructs for Monomer Reactivity Profiling

2005 • 25 citations

Solid-phase synthesis of α-substituted proline hydantoins and analogs

2005 • 25 citations

Reaction of α-iminomethylene amino esters with mono- and bidentate nucleophiles: a straightforward route to 2-amino-1H-5-imidazolones

2001 • 25 citations

A thermally-cleavable linker for solid-phase synthesis

2005 • 25 citations

Microwave-assisted synthesis of imidazoles: Reaction of p-toluenesulfonylmethyl isocyanide and polymer-bound imines

2005 • 25 citations

Synthesis of alkyl sulfonates from sulfonic acids or sodium sulfonates using solid-phase bound reagents

2001 • 25 citations

Microwave-assisted scavenging of electrophiles utilizing polymer-supported sequestration reagents. Application to the synthesis of N3-acylated dihydropyrimidine libraries

2003 • 25 citations

“Volatilizable” Supports for High-Throughput Organic Synthesis

2005 • 25 citations

Stereoselective Solid‐Phase Synthesis of Chiral Piperidine Derivatives by Using an Immobilized Galactose Auxiliary

2003 • 25 citations

Solid-phase synthesis of α-hydroxy phosphonates and hydroxystatine amides. Transition-state isosteres derived from resin-bound amino acid aldehydes

2001 • 25 citations

Synthesis of polymeric supports with spacer-modified triazene linkers: aldol and Grignard reactions of immobilized nortropinone

2003 • 24 citations

Synthesis and application of polytetrahydrofuran-grafted polystyrene (PS–PTHF) resin supports for organic synthesis

2005 • 24 citations

Preparation of a Kröhnke Pyridine Combinatorial Library Suitable for Solution-Phase Biological Screening

2003 • 24 citations

Convergent Solid-Phase Synthesis of Symmetrical Benzo[b]furan's Dimerizer

2002 • 24 citations

Parallel Solution-Phase Synthesis of 4-Dialkylamino-2-methylsulfonyl-6-vinylpyrimidines

2004 • 24 citations

FACILE MICROWAVE-ASSISTED ONE-POT SOLID PHASE SYNTHESIS OF SPIRO [3H-INDOLE-3,4'-PYRAZOLO[3,4-b] PYRIDINES]

2003 • 24 citations

The synthesis of potentially selective inhibitors of dihydroorotate dehydrogenase. The utilization of chemoselective Suzuki cross-coupling reactions in a parallel synthesis

2001 • 24 citations

2-Methoxy-6-oxo-1,4,5,6-tetrahydropyridine-3-carbonitriles: Versatile Starting Materials for the Synthesis of Libraries with Diverse Heterocyclic Scaffolds

2005 • 24 citations

Solid-phase synthesis of 2-amino-3-chloro-5- and 8-nitro-1,4-naphthoquinones: a new and general colorimetric test for resin-bound amines

2005 • 24 citations

Cleavage of immobilized disubstituted triazenes with electrophiles: solid-phase synthesis of alkyl halides and esters

2001 • 24 citations

Solid-Phase Synthesis of β-Amino Ketones and Six-Ring Carbamates via Immobilized α-Alkoxycarbonylamino Sulfones

2001 • 24 citations

One-Step Construction of Peptidomimetic 5-Carbamoyl-4-sulfonyl-2-piperazinones

2005 • 24 citations

Synthesis of 1-Alkyl-4-imidazolecarboxylates: A Catch and Release Strategy

2005 • 24 citations

Solid-phase synthesis of 3,7-disubstituted perhydro-1,4-diazepine-2,5-diones from amino acids and β-amino acids

2001 • 23 citations

Polymer-Supported Benzotriazoles as Catalysts in the Synthesis of Tetrahydroquinolines by Condensation of Aldehydes with Aromatic Amines

2001 • 23 citations

Novel 5-aryl-1,3-dihydro-indole-2-thiones

2003 • 23 citations

Lipase-Catalyzed Kinetic Resolution on Solid-Phase via a “Capture and Release” Strategy

2003 • 23 citations

Synthesis of a New Fluoro-Wang Resin for Solid-Phase Reaction Monitoring by ¹⁹F NMR Spectroscopy

2001 • 23 citations

Chemical library synthesis using convergent approaches

2005 • 23 citations

Efficient solid phase synthesis of benzo[1,2,3]thiadiazoles and related structures

2005 • 23 citations

Tentoxin as a Scaffold for Drug Discovery. Total Solid-Phase Synthesis of Tentoxin and a Library of Analogues

2003 • 23 citations

A forward-genetic approach for analysis of the immune system

2003 • 23 citations

Substituted aminobenzimidazole pyrimidines as cyclin-dependent kinase inhibitors

2005 • 23 citations

Solid-Phase Synthesis of Bis-Heterocyclic Compounds from Resin-Bound Orthogonally Protected Lysine

2000 • 23 citations

Procedure for the Parallel Preparation of 3-Imidazo[1,2-a]pyridin-3-yl-propionic Acid Derivatives Involving Meldrum's Acid

2005 • 22 citations

Synthesis of Bicyclic Pyrimidine Derivatives as ATP Analogues

2001 • 22 citations

Solid-phase synthesis of dehydropeptide, AM-toxin II, using a novel selenyl linker by side-chain tethered strategy

2001 • 22 citations

Solution-Phase and Solid-Phase Syntheses of Enzyme Inhibitor RK-682 and Antibiotic Agglomerins

2005 • 22 citations

Solid-phase combinatorial synthesis of polyamine derivatives using aminoalcohol building blocks

2001 • 22 citations

Chemical genomics as an emerging paradigm for postgenomic drug discovery

2003 • 22 citations

Amino Acid-Derived Heterocycles as Combinatorial Library Targets: Spirocyclic Ketal Lactones

2003 • 22 citations

Preparation of Resin-BoundN-(α-Methoxyalkyl)amides: An Advantageous Use of Solid-Phase Chemistry for the Handling of Unstable Precursors of the VersatileN-Acyliminium Ions

2001 • 22 citations

Polymer-Supported Triazole and Benzotriazole Leaving Groups. Three New Examples and a Comparison of Their Efficiency

2001 • 22 citations

Development of Low Molecular Weight HIV-1 Protease Dimerization Inhibitors

2004 • 22 citations

High‐resolution analysis of a 144‐membered pyrazole library from combinatorial solid phase synthesis by using electrospray ionisation Fourier transform ion cyclotron resonance mass spectrometry

2001 • 21 citations

The design of phenylglycine containing benzamidine carboxamides as potent and selective inhibitors of factor Xa

2001 • 21 citations

High-Throughput Purification of Single Compounds and Libraries

2005 • 21 citations

Solid Phase Synthesis of 2-Aminoquinazoline-Based Compounds

2003 • 21 citations

Oxidation–Cope elimination: a REM-resin cleavage protocol for the solid-phase synthesis of hydroxylamines

2001 • 21 citations

Bibliotheken niedermolekularerαvβ3-Integrinantagonisten: On-Bead-Screening und massenspektrometrische Identifizierung ohne Codierung

2001 • 21 citations

Adsorption‐Mediated Electrochemical Sensing of Halides

2001 • 21 citations

Solid-Phase Library Synthesis of Alkoxyprolines

2001 • 21 citations

Novel, selective indole-based ECE inhibitors: Lead optimization via solid-phase and classical synthesis

2005 • 21 citations

Parallel Solid-Phase Synthesis and Evaluation of Inhibitors of Streptomyces coelicolor Type II Dehydroquinase

2003 • 21 citations

A solid-phase version of the palladium-catalyzed carbonyl allylation by allylic alcohols with SnCl2

2001 • 21 citations

A Novel Approach for Solid-Phase Synthesis of Substituted Imidazolines and Bis-Imidazolines

2001 • 21 citations

Mechanism and structure–activity relationships of norspermidine-based peptidic inhibitors of trypanothione reductase

2005 • 21 citations

Efficient synthesis of 3-cyano-6-(2-hydroxyphenyl)pyridines by multi-component condensations on beads

2003 • 21 citations

Alkene Chemoselectivity in Ring-Closing Metathesis: A Formal Synthesis of (-)-Periplanone-B

1999 • 21 citations

Use of Quinolinium Salts in Parallel Synthesis for the Preparation of 4-Amino-2-alkyl-1,2,3,4-tetrahydroquinoline

2005 • 21 citations

One-pot synthesis of α-acyloxyaminoamides via nitrones as imine surrogates in the Ugi MCR

2005 • 21 citations

Convenient Preparation and Use of a New Analytical Construct for the Analysis and Development of Solid-Phase Chemistries

2003 • 20 citations

Strategy for the Synthesis of Polymeric Supports with Hydrazone Linkers for Solid-Phase Alkylation of Ketones and Aldehydes

2004 • 20 citations

Solid-Supported Benzotriazoles. 2. Synthetic Auxiliaries and Traceless Linkers for the Combinatorial Synthesis of Unsymmetrical Ureas

2001 • 20 citations

Solid-phase synthesis of 3-hydroxymethyl isoxazoles via resin bound nitrile oxides

2001 • 20 citations

A Novel Hydrazine Linker Resin and Its Application for the Solid-Phase Synthesis of α-Branched Primary Amines

2000 • 20 citations

Conformationally Constrained Analogues of Bleomycin A₅

2003 • 20 citations

Solid Phase Synthesis of Carbocyclic<scp>l</scp>-2‘-Deoxynucleosides

2001 • 20 citations

Combinatorial Synthesis of Heterocycles: Solid-Phase Synthesis of 6-Amino-2,4-dioxo-3,4-dihydro-1,3,5-triazine Derivatives

2001 • 20 citations

Solid-phase synthesis of 1,3-disubstituted 2-thioxoquinazoline-4-ones using SNAr reaction

2001 • 20 citations

Hydroformylation of Terminal Alkenes Supported on Solid Phase: Synthetic Tool for Combinatorial Chemistry

2003 • 20 citations

Directed Library of Anilinogeranyl Analogues of Farnesyl Diphosphate via Mixed Solid- and Solution-Phase Synthesis

2005 • 20 citations

Solution-Phase Parallel Synthesis of 115 Homosilatecan Analogues

2003 • 20 citations

The Manual and Automated Solid-Phase Synthesis of α-Substituted Prolines and Homologues

2003 • 19 citations

A Facile and Highly Efficient Route to a Traceless π-Arene Chromium Linker. Applications to Synthetic and Combinatorial Chemistry

2001 • 19 citations

Polymer-Supported 1,3-Oxazolium-5-olates: Synthesis of 1,2,4-Triazoles

2004 • 19 citations

Solution-phase parallel synthesis of 5-carboxamido 1-benzyl-3-(3-dimethylaminopropyloxy)-1H-pyrazoles as activators of soluble guanylate cyclase with improved oral bioavailability

2001 • 19 citations

Polymer-supported chiral phosphinooxazolidine ligands for palladium-catalyzed asymmetric allylic alkylations and Diels–Alder reactions

2005 • 19 citations

Solid-Phase Polyamine Synthesis Using Piperazine and Piperidine Building Blocks

2003 • 19 citations

Solid-phase synthesis of quinoxaline, thiazine, and oxazine analogs through a benzyne intermediate

2005 • 19 citations

Polymer-bound diazonium salts for the synthesis of diazoacetic esters

2005 • 19 citations

Rapid and efficient solid-supported reagent synthesis of fluorine derivatives of phosphorus(V) compounds

2005 • 19 citations

Cyclopropanation of 3,4-dihydro-1 H-benzo[e][1,4]diazepine-2,5-diones

2005 • 19 citations

Solid-phase synthesis of bis-cyclic guanidines from tripeptides

2001 • 19 citations

Base catalyzed intramolecular transamidation of 2-aminoquinazoline derivatives on solid phase

2005 • 19 citations

Microwave-Assisted “Libraries from Libraries” Approach toward the Synthesis of Allyl- and C-Cyclopropylalkylamides

2005 • 19 citations

Polystyrylsulfonyl chloride resin: an efficient solid-supported condensation reagent for the solution phase synthesis of esters

2001 • 19 citations

Recyclable supports for stereoselective 1,3-dipolar cycloadditions: application of a fluorous oxazolidinone chiral auxiliary

2005 • 19 citations

Trimellitic anhydride linker (TAL)—highly orthogonal conversions of primary amines employed in the parallel synthesis of labeled carbohydrate derivatives

2003 • 19 citations

Solid phase palladium-catalysed CC bond formation in the pyridine series: access to aryl and alkynyl pyridylpiperazines

2003 • 19 citations

A convenient parallel synthesis of low molecular weight hydroxamic acids using polymer-supported 1-hydroxybenzotriazole

2003 • 19 citations

Synthesis of 3,4‐Dihydropyrimidine‐2(1H)‐thiones and Quinazolin‐4(3H)‐ones over Yb(III)‐Resin Catalyst Under Solvent‐free Conditions

2005 • 19 citations

A Novel Solid-Phase Approach to 2,4-Diaminothiazoles

2000 • 19 citations

A post-Ugi carbonylation/intramolecular amidation approach toward the synthesis of macrolactams

2005 • 19 citations

Design and Synthesis of 4-Substituted Benzamides as Potent, Selective, and Orally Bioavailable I_Ks Blockers

2001 • 18 citations

Application of Aryloximes as Solid-Phase Ketone Linkers

2002 • 18 citations

N-Benzoyl amino acids as LFA-1/ICAM inhibitors 1: amino acid structure–activity relationship

2003 • 18 citations

BAL resin for the preparation of secondary amines

2003 • 18 citations

Traceless, Self-Cleaving Solid- and Solution-Phase Parallel Synthesis of 3,4,7-Trisubstituted 3,4-Dihydroquinoxalin-2-ones

2001 • 18 citations

Solid-phase synthesis of a focused library of trypanothione reductase inhibitors

2003 • 18 citations

Design and Synthesis of a Maximally Diverse and Druglike Screening Library Using REM Resin Methodology

2001 • 18 citations

ROMPgel Beads in IRORI Format: Acylations Revisited

2004 • 18 citations

Oxetane synthesis via cyclisation of aryl sulfonate esters on polystyrene and PEG polymeric supports

2004 • 18 citations

Solid phase synthesis of enantiomerically pure polyhydroxyvalerolactams

2001 • 18 citations

Abnormal aza-Wittig reaction on the solid-phase: chemoselectivity studies towards the parallel synthesis of 3-aryl-2,4-dioxo-1,3,5-triazino[1,2-a]benzimidazoles

2003 • 18 citations

The development and preparation of the 2,4-dimethoxybenzyl arylhydrazine (DMBAH) “latent” safety-catch linker: solid phase synthesis of ketopiperazines

2003 • 18 citations

A New Supported Reagent for the Parallel Synthesis of Primary and SecondaryO-Alkyl Hydroxylamines through a Base-Catalyzed Mitsunobu Reaction

2005 • 18 citations

Combinatorial synthesis of libraries of indole derivatives

2001 • 18 citations

Oligomeric ethylene glycols as sorting tags for parallel and combinatorial mixture synthesis

2005 • 18 citations

A modular approach to the SPOT synthesis of 1,3,5-trisubstituted hydantoins on cellulose membranes

2001 • 18 citations

Diaryl ether inhibitors of farnesyl-protein transferase

2001 • 18 citations

Efficient solid-phase synthesis of quinazoline-2,4-diones with various substituents on aromatic rings

2003 • 18 citations

Identification of potent and broad-Spectrum antibiotics from SAR studies of a synthetic vancomycin analogue

2003 • 18 citations

DNA Transfection Screening from Single Beads

2004 • 18 citations

PS-COD and PS-9-BBN: Polymer-Supported Reagents for Solution-Phase Parallel Synthesis

2005 • 17 citations

Westphal Reaction in Solid-Phase

2003 • 17 citations

Discovery of AICAR Tfase inhibitors that disrupt requisite enzyme dimerization

2005 • 17 citations

The Preparation of a New “Safety Catch” Ester Linker for Solid-Phase Synthesis

2001 • 17 citations

Preparation of 2- and 4-Arylmethyl N-Substituted and N,N-Disubstituted Anilines via a “Green”, Multicomponent Reaction

2005 • 17 citations

Forward &amp; Reverse Chemical Genetics Using SPOS-Based Combinatorial Chemistry

2003 • 17 citations

Parallel solid-phase synthesis and characterization of new sulfonamide and carboxamide proline derivatives as potential CNS agents

2005 • 17 citations

Deazapurine Solid-Phase Synthesis: Combinatorial Synthesis of a Library of N3,N5,C6-Trisubstituted Pyrrolo[3,2-d]pyrimidine Derivatives on Cross-Linked Polystyrene Bearing a Cysteamine Linker

2005 • 17 citations

Solution-Phase Parallel Wittig Olefination: Synthesis of Substituted 1,2-Diarylethanes

2003 • 17 citations

Construction of a 2,6-Difunctionalized 2-Methyl-2H-1-benzopyran Library by Using a Solid-Phase Synthesis Protocol

2005 • 17 citations

Urea small molecule agonists on mouse melanocortin receptors

2003 • 17 citations

Efficient Microwave Combinatorial Parallel and Nonparallel Synthesis of N-Alkylated Glycine Methyl Esters as Peptide Building Blocks

2005 • 17 citations

Solid-Phase Directed Ortho-Lithiation and the Preparation of a Phthalide Library

2001 • 17 citations

A novel solid-phase synthesis of di- and trisubstituted N-acyl ureas

2003 • 17 citations

Alkene epoxidation with urea–hydrogen peroxide complex and PS–DVB supported phthalic anhydride

2005 • 17 citations

Nipecotic and iso -nipecotic amides as potent and selective somatostatin subtype-2 receptor agonists

2001 • 17 citations

Solution-Phase Parallel Synthesis of Spirohydantoins

2004 • 16 citations

Solid-Phase Synthesis of Benzoxazoles from 3-Nitrotyrosine

2001 • 16 citations

Solid-Phase Syntheses of 6-Arylpyridazin-3(2H)-Ones

2005 • 16 citations

Solid-phase synthesis of substituted 3-amino-3′-carboxy-tetrahydrocarbazoles

2004 • 16 citations

Solid-phase synthesis of imidazoquinazolinone derivatives with three-point diversity

2004 • 16 citations

An Efficient Synthesis of Gougerotin and Related Analogues Using Solid- and Solution-Phase Methodology

2005 • 16 citations

Solid-phase aldol condensations mediated by zinc acetate and 2,2′-bipyridine under weakly basic conditions

2003 • 16 citations

A Three‐Dimensional Array for Multiparallel Synthesis

2003 • 16 citations

Solid-phase domino syntheses of functionalized tetronates with Ph3PCCO

2003 • 16 citations

Parallel iterative solution-phase synthesis of 5-amino-1-aryl-[1,2,4]triazolo[1,5-a]pyridine-7-carboxylic acid amide derivatives

2003 • 16 citations

Lipophilic versus hydrogen-bonding effect in P3 on potency and selectivity of valine aspartyl ketones as caspase 3 inhibitors

2005 • 16 citations

Fluorocarbon accelerated supported transformations (FAST) on REM resin

2001 • 16 citations

Solid-Phase Synthesis of 2,4-Diaminoquinazoline Libraries

2001 • 16 citations

Parallel modification of tropane alkaloids

2001 • 16 citations

Capture-ROMP-release: application to the synthesis of amines and alkyl hydrazines

2003 • 16 citations

Solid-Phase Synthesis of Cleavable N-Arylmaleimides: Applications in 1,3-Dipolar Cycloaddition and in Thiol Scavenging

2001 • 15 citations

Isomeric thiazole derivatives as ligands for the neuropeptide Y5 receptor

2005 • 15 citations

Microwave assisted solid-phase synthesis of trisubstituted 2-(2,6-purin-9-yl)acetamides

2005 • 15 citations

Palladium-catalysed nucleophilic release of allylic amines from a phenolic resin

2001 • 15 citations

The Solid-Phase Synthesis and Use of N-Monosubstituted Piperazines in Chemical Library Synthesis

2003 • 15 citations

Synthesis of cyclic peptidosulfonamides as scaffolds for MC4 pharmacophoric groups

2004 • 15 citations

Solid-phase lithiation of 5-carboxyindoles

2003 • 15 citations

Trityl Isothiocyanate Support for Solid-Phase Synthesis

2000 • 15 citations

Solid-Phase Synthesis of 7-Acylamino-1,4-benzodiazepine-2,5-diones

2003 • 15 citations

Pyrazolyl–benzoxazole derivatives as protein kinase inhibitors. Design and validation of a combinatorial library

2005 • 15 citations

Spiroimidazolidinone Library Derivatives on SynPhase Lanterns

2003 • 15 citations

Versatile Solid-Phase Synthesis of Trisubstituted 1H-Pyrido[2,3-d]pyrimidin-4-ones and Related Heterocycles

2004 • 15 citations

A concise synthesis of ortho-substituted aryl-acrylamides—potent activators of soluble guanylyl cyclase

2003 • 15 citations

Efficient solid-phase synthesis of 4,5-dihydro-1,2,4-triazin-6(1H)-ones

2003 • 15 citations

Solid-phase optimisation of achiral amidinobenzyl indoles as potent and selective factor Xa inhibitors

2001 • 15 citations

2,6-Diketopiperazines from Amino Acids, from Solution-Phase to Solid-Phase Organic Synthesis

2001 • 15 citations

Synthesis of New 3‘-, 5-, andN⁴-Modified 2‘-O-Methylcytidine Libraries on Solid Support

2003 • 14 citations

Vilsmeier Formylation of 2-Carboxyindoles and Preparation of O-Benzylhydroxyureas on Solid Phase

2001 • 14 citations

Novel HIV-1 protease inhibitors active against multiple PI-Resistant viral strains: coadministration with indinavir

2003 • 14 citations

Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors

2005 • 14 citations

A New Linker for Anchoring/Masking Primary Amines on Solid Support

2005 • 14 citations

Efficient approach for the diversity-oriented synthesis of macro-heterocycles on solid-support

2003 • 14 citations

A new bio-compatible pH cleavable linker for solid-phase synthesis of a squalamine analogue

2001 • 14 citations

Development of resin-to-resin transfer reactions (RRTR) using Sonogashira chemistry

2005 • 14 citations

A novel synthesis of polysubstituted naphthalenes

2001 • 14 citations

Polymer-Supported Haloarene Chromium Dicarbonyl Isonitrile Complexes: A Study of Their Synthesis and Reactivity

2003 • 13 citations

Chemical Genomics Strategy for the Discovery of New Anticancer Agents

2003 • 13 citations

N-[Chloro(dimethylamino)methylene]-N-methylmethanaminium chloride (TMUCl Cl), the reagent of choice for the solid-phase synthesis of anilides

2005 • 13 citations

Poly(ethylene glycol)-supported copper(II) triazacyclononane: an efficient, recoverable, and recyclable catalyst for the cleavage of a phosphodiester

2003 • 13 citations

Expedited discovery of second generation NK-1 antagonists: identification of a nonbasic aryloxy substituent

2001 • 13 citations

A convenient ‘catch and release’ synthesis of fused 2-alkylthio-pyrimidinones mediated by polymer-bound BEMP

2003 • 13 citations

Combinatorial Solid-Phase Synthesis of 6-Hydroxy-1,2,3,4-tetrahydro-β-carbolines from <scp>l</scp>-5-Hydroxytryptophan

2005 • 13 citations

Parallel synthesis of 4-amino-2,6-dialkylamino-pyridines

2003 • 13 citations

Parallel Liquid-Phase Synthesis of N-Substituted 6-Aminosulfonyl-2-oxo-1,2-dihydroquinoline-4-carboxamide and 6-Aminosulfonylquinoline-4-carboxamide Derivatives

2004 • 13 citations

Versatile solid-phase synthesis of secondary amines from alcohols. Development of an N-Boc-(o-nitrobenzene)sulfonamide linker

2003 • 13 citations

Identification of TNF-α inhibitors from a split-Pool library based on a tyrosine-Proline peptidomimetic scaffold

2003 • 13 citations

Parallel synthesis of 4,5-dihydro-1H-1,4-benzodiazepine-2,3-diones

2001 • 12 citations

Directed ortho Metalation Reaction of Aryl O-Carbamates on Solid Support

2005 • 12 citations

Synthesis and evaluation of cis-hexahydropyrrolo[3,2-b]pyrrol-3-one peptidomimetic inhibitors of CAC1 cysteinyl proteinases

2004 • 12 citations

N-(3-Phenylsulfonyl-3-piperidinoyl)-phenylalanine derivatives as potent, selective VLA-4 antagonists

2003 • 12 citations

Liquid-phase synthesis of mixture-based bicyclic β-lactam libraries

2003 • 12 citations

Highly potent and selective αVβ3-receptor antagonists: solid-phase synthesis and SAR of 1-substituted 4-amino-1H-pyrimidin-2-ones

2003 • 12 citations

Solid-phase synthesis of unsymmetrical ureas through the use of Kenner safety-catch linker

2003 • 12 citations

Solid‐phase synthesis of a novel series of 2,3,4,5‐tetrahydro‐1,4‐benzodiazepin‐2,5‐dione libraries

2003 • 12 citations

Solid-phase synthesis of pyrido[2,3-d]pyrimidin-7-ones

2005 • 12 citations

Evaluation of Solution and Solid-Phase Approaches to the Synthesis of Libraries of α,α-Disubstituted-α-acylaminoketones

2005 • 12 citations

Diamine containing VLA-4 antagonists

2001 • 12 citations

Tablets of Functionalized Polystyrene Beads Alone and in Combination with Solid Reagents or Catalysts. Preparation and Applications in Parallel Solution and Solid Phase Synthesis

2003 • 12 citations

Hetero Diels–Alder reactions (HDAR) of α,α′-dioxothiones on solid support

2005 • 12 citations

Application of a Photolabile Backbone Amide Linker for Cleavage of Internal Amides in the Synthesis towards Melanocortin Subtype‐4 Agonists

2005 • 12 citations

O,N,N‘-Trialkylisoureas as Mild Activating Reagents for N-Acylsulfonamide Anchors

2005 • 12 citations

Enantioselective Synthesis of Linear Polypropionate Arrays Using Anthracene-Tagged Organosilanes

2005 • 12 citations

Discovery of 2-Aminothiazole-4-carboxamides, a Novel Class of Muscarinic M3 Selective Antagonists, through Solution-Phase Parallel Synthesis

2005 • 12 citations

Inhibitory activity of a ceramide library on interleukin-4 production from activated T cells

2005 • 11 citations

Development of Cross-Linked Polystyrene-Supported Chiral Amines Featuring a Fluorinated Linker for Gel-Phase ¹⁹F NMR Spectrometry Monitoring of Reactions

2005 • 11 citations

Solid-phase synthesis of model libraries of 3 ?17?-dihydroxy-16?-(aminoethyl-N-substituted)-5?-androstanes for the development of steroidal therapeutic agents

2005 • 11 citations

Preparation of Resin-Bound Bismethylene Cyclic Malonic Acid Ester and Facile Solid-Phase Synthesis of 2-Alkylthio-4(1H)-quinolone and 2-Alkyl-4(1H)-quinolone

2003 • 11 citations

Preparation of a novel polystyrene-based urea resin

2005 • 11 citations

Combinatorial synthesis of SSAO inhibitors using sonogashira coupling: SAR of aryl propargylic amines

2001 • 11 citations

Solid-Phase Synthesis of Structurally Diverse 2-Alkyl- and 2-Aryl-Pyrimidines from Support-Bound Amidines

2005 • 11 citations

The Solid-Phase Nicholas Reaction: Scope and Limitations

2005 • 11 citations

Polystyrylsulfonyl-3-nitro-1H-1,2,4-triazolide-resin: a new solid-supported reagent for the esterification of amino acids

2003 • 11 citations

Design and Synthesis of A Diverse Morpholine Template Library

2003 • 11 citations

Solid-phase synthesis of 1-substituted 4,5-dihydro-1,2,4-triazin-6-ones

2001 • 11 citations

Solid-phase Bromination and Suzuki Coupling of 2-Carboxyindoles

2001 • 11 citations

Michael addition of amines to vinyl sulfonamides on solid support

2001 • 11 citations

Stereoselective Methodology for 1-Aryl-1-alkyl Epoxides via Chromium Tricarbonyl Complexes

2004 • 11 citations

Rapid access to reactive polymer-supported isocyanates

2004 • 10 citations

Solid phase synthesis of trypanothione reductase inhibitors—towards single bead screening

2001 • 10 citations

Solid-phase synthesis of a type II′ β-turn peptido-mimetic library

2003 • 10 citations

Stereoselective Hydrogenation of Tetrasubstituted Enones

2004 • 10 citations

Solid-Phase Combinatorial Library of Norstatine-Type Isosters by the Nitroaldol Reaction

2003 • 10 citations

Solid-phase synthesis of acyl biarylsulfonamides

2001 • 10 citations

Cross coupling reactions of organozinc iodides with solid-supported electrophiles: synthesis of 4-substituted benzoic and 3-substituted (E)- and (Z)-propenoic acids and amides

2002 • 9 citations

Regioselective solid-phase 4-amino-de-chlorination of 2,4,6-trichloropyrimidine by resin-supported N -potassium carbamates

2001 • 9 citations

A Highly Automated, Polymer-Assisted Strategy for the Preparation of 2-Alkylthiobenzimidazoles and N,N‘-Dialkylbenzimidazolin-2-ones

2005 • 9 citations

An improved two-resin method for the cleavage of tertiary amines from REM resin

2001 • 9 citations

Expanding the Chemical Diversity of Azinone Libraries by A Consecutive Alkylation/Palladium-Catalyzed Functionalization Strategy

2005 • 9 citations

4-Amino-2-(aryl)-butylbenzamides and Their conformationally constrained analogues. Potent antagonists of the human neurokinin-2 (NK2) receptor

2003 • 9 citations

Synthesis and evaluation of a novel series of farnesyl protein transferase inhibitors as non-peptidic CAAX tetrapeptide analogues

2003 • 9 citations

Natural Products as Scaffolds for Chemical Diversification: Solution-Phase Parallel Synthesis of a Series of Naringin Analogues

2005 • 9 citations

Random Chemistry as a New Tool for the Generation of Small Compound Libraries: Development of a New Acetylcholinesterase Inhibitor

2005 • 9 citations

A Chiral Cyclohexanone Linked to Polystyrene for Solid-Phase Synthesis of Chiral α-Carbonyls

2005 • 9 citations

Solid-phase synthesis of functionalized tropane derivatives via 1,3-dipolar cycloaddition

2001 • 9 citations

Solid-phase synthesis and biochemical evaluation of conformationally constrained analogues of deglycobleomycin A 5

2003 • 9 citations

Solvomercuration and demercuration of alkenes on solid-phase

2001 • 8 citations

Initial Structure-Activity Relationships for a Caprolactam-based Series of Neutral Factor Xa Inhibitors: Lead Identification

2005 • 8 citations

Expeditious solution phase synthesis of fluoroquinolone antibacterial agents using polymer supported reagents

2001 • 8 citations

A Combinatorial Approach toward the Generation of Ambiphilic Peptide-Based Inhibitors of Protein:Geranylgeranyl Transferase-1

2005 • 8 citations

Carbon−Carbon and Carbon−Heteroatom Bond Formation on Solid Phase Using Cationic Iron Carbonyl Complexes

2005 • 8 citations

Solid Phase Oxidation of Alcohols and Benzyl Halides to Carbonyls Using Bromate Exchange Resin

2003 • 8 citations

Solid- and solution-Phase synthesis of highly-Substituted-Pyrrolidine libraries

2001 • 8 citations

Syntheses of 5-Oxa-10,11-diazadibenzo[a,d]cycloheptenes on Solid Supports

2005 • 8 citations

Optimization of spiroimidazolidinone derivatives synthesis on solid phase using SynPhase™ Lanterns

2003 • 8 citations

Solid-phase synthesis of 2-substituted 4-amino-7-oxo-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidines: an example of cyclization-assisted cleavage.

2003 • 8 citations

Preparation of potential inhibitors of the mur-Pathway enzymes on solid support using an acetal linker

2003 • 7 citations

Synthesis of dehydroalanine fragments as thiostrepton side chain mimetics

2005 • 6 citations

From pure FPP to mixed FPP and CAAX competitive inhibitors of farnesyl protein transferase

2003 • 6 citations

Selective Polymer‐Assisted Product Sequestration for the Generation of Combinatorial Libraries of 1,3‐Thiazines

2005 • 6 citations

The Traceless Solid-Phase Synthesis of Organic Molecules

2003 • 6 citations

A Blue Dye for Substrate Tagging in the Two-Color Screening of Combinatorial Libraries

2004 • 6 citations

Solution-phase parallel synthesis of substituted 1,2-ethyl and 1,3-propyl diamines

2003 • 6 citations

Solid-phase synthesis of 2,3-diphenylpropionic acid library as VLA-4 antagonists

2005 • 5 citations

Solid-Phase Synthesis of a 6-Phenylquinolin-2(1H)-one Library Directed toward Nuclear Hormone Receptors

2005 • 5 citations

Communication: Polymer-Assisted Solution-Phase Synthesis of 4,5-Dihydro- 1,4-Benzoxazepin-3(2H)-Ones

2005 • 5 citations

( R )-3-( N -Methylpyrrolidin-2-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives as high affinity h5-HT 1B/1D ligands

2003 • 5 citations

The Design, Synthesis and Screening of a Muscarinic Acetylcholine Receptor Targeted Compound Library

2005 • 5 citations

Cleavage of Oximes Using a Solid Supported Hypervalent Organoiodine Reagent

2005 • 5 citations

Simple Tools for Resin Distribution

2004 • 5 citations

A Parallel Synthesis Demonstration Library of Tri-Substituted Indazoles Containing New Antimutagenic / Antioxidant Hits Related to Benzydamine

2003 • 5 citations

Optimization of CRF1R binding affinity of 2-(2,4,6-trichlorophenyl)-4-trifluoromethyl-5-aminomethylthiazoles through rapid and selective parallel synthesis

2004 • 5 citations

Recycling solid supports--a head-to-tail linker.

2003 • 3 citations

Naked-Eye Bead Property Estimation Using a Red Safety-Catch Linker

2005 • 3 citations

Chloromethoxymethyl Polystyrene (CMM Resin), an Acid Labile Resin for Anchoring/Cleavage of N-Heterocycles and Oxygen Aromatic Compounds

2005 • 3 citations

Identification of Privileged Scaffolds from a Diversified Chemical Library for&amp;#946;-Secretase Inhibition

2005 • 3 citations