Design and Synthesis of Lipophilic Phosphoramidate d4T-MP Prodrugs Expressing High Potency Against HIV in Cell Culture: Structural Determinants for in Vitro Activity and QSAR

3'-Azido-3'-deoxythymidine (BW A509U): an antiviral agent that inhibits the infectivity and cytopathic effect of human T-lymphotropic virus type III/lymphadenopathy-associated virus in vitro.

1985 • 1,830 citations

Phosphorylation of 3'-azido-3'-deoxythymidine and selective interaction of the 5'-triphosphate with human immunodeficiency virus reverse transcriptase.

1986 • 1,348 citations

Aromatic substituent constants for structure-activity correlations

1973 • 1,189 citations

Inhibition of the in vitro infectivity and cytopathic effect of human T-lymphotrophic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV) by 2',3'-dideoxynucleosides.

1986 • 1,032 citations

Utilization of operational schemes for analog synthesis in drug design

1972 • 435 citations

Both 2′,3′-dideoxythymidine and its 2′,3′-unsaturated derivative (2′,3′-dideoxythymidinene) are potent and selective inhibitors of human immunodeficiency virus replication in vitro

1987 • 340 citations

Differential Patterns of Intracellular Metabolism of 2′,3′-Didehydro-2′,3′-dideoxythymidine and 3′-Azido-2′,3′-dideoxythymidine, Two Potent Anti-human Immunodeficiency Virus Compounds

1989 • 340 citations

3'-Substituted 2',3'-dideoxynucleoside analogs as potential anti-HIV (HTLV-III/LAV) agents

1987 • 294 citations

In search of a selective antiviral chemotherapy

1997 • 236 citations

The anti-HTLV-III (anti-HIV) and cytotoxic activity of 2',3'-didehydro-2',3'-dideoxyribonucleosides: a comparison with their parental 2',3'-dideoxyribonucleosides.

1987 • 226 citations

Aryl Phosphoramidate Derivatives of d4T Have Improved Anti-HIV Efficacy in Tissue Culture and May Act by the Generation of a Novel Intracellular Metabolite

1996 • 220 citations

1-(2,3-Dideoxy-.beta.-D-glycero-pent-2-enofuranosyl)thymine. A highly potent and selective anti-HIV agent

1989 • 216 citations

Cellular metabolism of 2',3'-dideoxycytidine, a compound active against human immunodeficiency virus in vitro.

1987 • 210 citations

Intracellular delivery of bioactive AZT nucleotides by aryl phosphate derivatives of AZT

1993 • 204 citations

Anti-retrovirus activity of 3′-fluoro- and 3′-azido-substituted pyrimidine 2′,3′-dideoxynucleoside analogues

1988 • 188 citations

Phosphorylation of 2',3'-dideoxyinosine by cytosolic 5'-nucleotidase of human lymphoid cells.

1989 • 176 citations

Minireview: nucleotide prodrugs

1995 • 130 citations

Metabolic pathways for the activation of the antiretroviral agent 2',3'-dideoxyadenosine in human lymphoid cells.

1988 • 123 citations

Pro-Nucleotides - Recent Advances in the Design of Efficient Tools for the Delivery of Biologically Active Nucleoside Monophosphates

1998 • 111 citations

Decomposition Pathways and in Vitro HIV Inhibitory Effects of IsoddA Pronucleotides: Toward a Rational Approach for Intracellular Delivery of Nucleoside 5‘-Monophosphates

1996 • 92 citations

The Presence of Substituents on the Aryl Moiety of the Aryl Phosphoramidate Derivative of d4T Enhances Anti-HIV Efficacy in Cell Culture: A Structure−Activity Relationship

1999 • 75 citations

2',3'-Dideoxycytidine: regulation of its metabolism and anti-retroviral potency by natural pyrimidine nucleosides and by inhibitors of pyrimidine nucleotide synthesis.

1987 • 73 citations

Conversion of 2′,3′‐dideoxyadenosine (ddA) and 2′,3′‐didehydro‐2′,3′‐dideoxyadenosine (d4A) to their corresponding aryloxyphosphoramidate derivatives markedly potentiates their activity against human immunodeficiency virus and hepatitis B virus

1997 • 61 citations

Relation of structures and microbiological activities of the 16-membered macrolides

1972 • 58 citations

Quantitative relationship between protonophoric and uncoupling activities of substituted phenols

1987 • 57 citations

Phosphoramidate derivatives of d4T with improved anti-HIV efficacy retain full activity in thymidine kinase-deficient cells

1996 • 55 citations

Nucleosides. XXXI. 3'-Amino-3'-deoxyhexopyranosyl Nucleosides. IV. Nucleoside Conversions in the 3'-Aminohexose Series¹

1966 • 27 citations

Phosphoramidates as Potent Prodrugs of anti-HIV Nucleotides: Studies in the Amino Region

1996 • 12 citations

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