Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10588356 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
We report herein the synthesis of a series of 3-hydroxyquinolin-2(1H)-one derivatives. Esters and amide groups were introduced at position 4 of the basis scaffold and some modulations of the benzenic moiety were performed. Most compounds presented selective inhibitory properties in the 10-20 μM range against HIV-1 reverse transcriptase associated ribonuclease H activity, without affecting the integrase and reverse transcriptase DNA polymerase activities. Unfortunately all tested compounds exhibited high cellular cytotoxicity in cell culture which limited their applications as antiviral agents.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Virginie Suchaud, Fabrice Bailly, Cédric Lion, Enzo Tramontano, Francesca Esposito, Angela Corona, Frauke Christ, Zeger Debyser, Philippe Cotelle,