| Literature DB >> 16023859 |
Vanessa Escuret1, Vincent Aucagne, Nicolas Joubert, David Durantel, Kimberly L Rapp, Raymond F Schinazi, Fabien Zoulim, Luigi A Agrofoglio.
Abstract
In this article, we report the synthesis of hitherto unknown 5-haloethynyl and 5-(1,2-dihalo)vinyluracil nucleosides in the 2'-deoxy, 3'-deoxy- and ribosyl series, and we discuss their in vitro anti-HIV and anti-HCV activities and cellular toxicitites. As a result, on the basis of their selectivity index (SI) obtained with the HCV replicon system, but also on their cytotoxicity on peripheral blood mononuclear, CEM and VERO cell lines, the best compounds were the 5-bromoethynyluridine (SI = 3.2) and the 5-(1-chloro-2-iodo)vinyluridine (SI > 2.8).Entities:
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Year: 2005 PMID： 16023859 DOI： 10.1016/j.bmc.2005.06.021
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641