Recent developments in the design of bioreductive drugs.

SR 4233 (Tirapazamine): a new anticancer drug exploiting hypoxia in solid tumours

1993 • 354 citations

Designed Enediynes: A New Class of DNA-Cleaving Molecules with Potent and Selective Anticancer Activity

1992 • 318 citations

Therapeutic attack of hypoxic cells of solid tumors: presidential address.

1988 • 258 citations

DT-diaphorase in activation and detoxification of quinones

1993 • 188 citations

Hypoxia-selective antitumor agents. 7. Metal complexes of aliphatic mustards as a new class of hypoxia-selective cytotoxins. Synthesis and evaluation of cobalt(III) complexes of bidentate mustards

1993 • 183 citations

The experimental development of bioreductive drugs and their role in cancer therapy

1993 • 137 citations

Considerations for the design of nitrophenyl mustards as agents with selective toxicity for hypoxic tumor cells

1986 • 129 citations

Hypoxia-Selective Agents Derived from Quinoxaline 1,4-Di-N-oxides

1995 • 121 citations

Self-Immolative Prodrugs: Candidates for Antibody-Directed Enzyme Prodrug Therapy in Conjunction with a Nitroreductase Enzyme

1994 • 114 citations

The bioactivation of CB 1954 and its use as a prodrug in antibody-directed enzyme prodrug therapy (ADEPT)

1993 • 107 citations

Cytotoxicity and antitumor activity of carzelesin, a prodrug cyclopropylpyrroloindole analogue.

1992 • 93 citations

Cellular Uptake of Misonidazole and Analogues with Acidic or Basic Functions

1985 • 93 citations

AQ4N: an alkylaminoanthraquinone N-oxide showing bioreductive potential and positive interaction with radiation in vivo

1995 • 87 citations

Hypoxia-selective antitumor agents. 3. Relationships between structure and cytotoxicity against cultured tumor cells for substituted N,N-bis(2-chloroethyl)anilines

1990 • 87 citations

DNA-directed alkylating agents. 1. Structure-activity relationships for acridine-linked aniline mustards: consequences of varying the reactivity of the mustard

1990 • 78 citations

Hypoxia-selective antitumor agents. 5. Synthesis of water-soluble nitroaniline mustards with selective cytotoxicity for hypoxic mammalian cells

1992 • 75 citations

Bioreducible mustards: a paradigm for hypoxia-selective prodrugs of diffusible cytotoxins (HPDCs)

1993 • 72 citations

Bioreductive drugs for cancer therapy: The search for tumor specificity

1994 • 72 citations

Structure-activity studies of benzimidazole-based DNA-cleaving agents. Comparison of benzimidazole, pyrrolobenzimidazole, and tetrahydropyridobenzimidazole analogs

1994 • 67 citations

Reductive Chemistry of the Novel Hypoxia-Selective Cytotoxin 5-[N,N-Bis(2-chloroethyl)amino]-2,4-dinitrobenzamide

1995 • 56 citations

Pyrrolo[1,2-a]benzimidazole-Based Quinones and Iminoquinones. The Role of the 3-Substituent on Cytotoxicity

1995 • 48 citations

In vitro cytotoxicity of GC sequence directed alkylating agents related to distamycin

1993 • 47 citations

Relationships between structure and kinetics of cyclization of 2-aminoaryl amides: potential prodrugs of cyclization-activated aromatic mustards

1994 • 41 citations

Chemosensitivity to the indoloquinone EO9 is correlated with DT-diaphorase activity and its gene expression

1994 • 37 citations

1-(5'-Fluoro-6'-hydroxy-5',6'-dihydrouracil-5'-yl)-5-fluorouracil, a novel N(1)-C(5)-linked dimer that releases 5-fluorouracil by radiation activation under hypoxic conditions

1992 • 36 citations

Tertiary amine N-oxides as bioreductive drugs: DACA N-oxide, nitracrine N-oxide and AQ4N.

1996 • 35 citations

Hypoxia-selective antitumor agents. 6. 4-(Alkylamino)nitroquinolines: a new class of hypoxia-selective cytotoxins

1992 • 34 citations

Nitroheterocycle reduction as a paradigm for intramolecular catalysis of drug delivery to hypoxic cells

1991 • 33 citations

Aliphatic amine N-oxides of DNA binding agents as bioreductive drugs.

1994 • 32 citations

NLA-1 : A 2-nitroimidazole radiosensitizer targeted to DNA by intercalation

1992 • 28 citations

Nitrobenzyl mustard quaternary salts: A new class of hypoxia-selective cytotoxins capable of releasing diffusible cytotoxins on bioreduction

1994 • 24 citations

Cyclopropamitosenes

1994 • 19 citations

Oxygen dependence of the cytotoxicity of the enediyne anti-tumour antibiotic esperamicin A1.

1996 • 17 citations

Nitrobenzyl derivatives as bioreductive alkylating agents: evidence for the reductive formation of a reactive intermediate

1986 • 17 citations

Clinical studies with EO9, a new indoloquinone bioreductive alkylating cytotoxic agent. EORTC Early Clinical Trials Group.

1994 • 15 citations

DNA-DNA Interstrand Crosslinking by 2,5-Bis(1-aziridinyl)-3,6-bis(carbethoxyamino)-1,4-benzoquinone: Covalent Structure of the dG-to-dG Cross-Links in Calf Thymus DNA and a Synthetic DNA Duplex

1994 • 14 citations

Fused pyrazine mono-N-oxides as bioreductive drugs III. Characterization of RB 90740 in vitro and in vivo

1995 • 14 citations

Pulse radiolysis studies on the hypoxia-selective toxicity of a colbalt-mustard complex.

1996 • 12 citations

Radiosensitization and Hypoxic Cell Toxicity of NLA‐1 and NLA‐2, Two New Bioreductive Compounds

1992 • 12 citations

Does DNA targeting affect the cytotoxicity and cell uptake of basic nitroquinoline bioreductive drugs?

1994 • 10 citations