Rational design of a new series of pronucleotide

A new pronucleotide series is described involving a two-step degradation process mediated by, respectively, carboxylesterase and phosphoramidase. Taking AZT as nucleosidyl moiety, it is shown that most of the compounds inhibit HIV replication in TK − cell line, which proves 5′-AZTMP delivery. A new...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2001-07, Vol.11 (13), p.1775-1777
Main Authors: Beltran, Thierry, Egron, David, Pompon, Alain, Lefebvre, Isabelle, Périgaud, Christian, Gosselin, Gilles, Aubertin, Anne-Marie, Imbach, Jean-Louis
Format: Article
Language:English
Subjects:
Anti-HIV Agents - chemical synthesis
Anti-HIV Agents - chemistry
Anti-HIV Agents - pharmacology
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Biological and medical sciences
Chromatography, High Pressure Liquid
Drug Design
HIV - physiology
Medical sciences
Nucleotides - chemistry
Nucleotides - pharmacology
Pharmacology. Drug treatments
Prodrugs - chemistry
Prodrugs - pharmacology
Virus Replication - drug effects
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Summary:A new pronucleotide series is described involving a two-step degradation process mediated by, respectively, carboxylesterase and phosphoramidase. Taking AZT as nucleosidyl moiety, it is shown that most of the compounds inhibit HIV replication in TK − cell line, which proves 5′-AZTMP delivery. A new pronucleotide series is described involving a two-step degradation process mediated by, respectively, carboxylesterase and phosphoramidase. Taking AZT as the nucleosidyl moiety, it is shown that most of the compounds inhibit HIV replication in the TK − cell line, which proves 5′-AZTMP delivery.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00299-2