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Selective inhibition of Human Immunodeficiency Virus type 1 (HIV-1) by a novel family of tricyclic nucleosides

AuthorsBonache, María-Cruz ; Cordeiro, Alessandra ; Quesada, Ernesto ; Vanstreels, Els; Daelemans, Dirk; Camarasa Rius, María José ; Balzarini, Jan; San-Félix, Ana
KeywordsAntiviral agents
HIV-1 reverse transcriptase inhibitors
Issue Date2011
CitationAntiviral Research 92 : 37–44 (2011)
AbstractNucleoside 1, with an unusual tricyclic carbohydrate moiety, specifically inhibits HIV-1 replication while being inactive against HIV-2 or other (retro) viruses. In an attempt to increase the inhibitory efficacy against HIV-1, and to further explore the structural features required for anti-HIV-1 activity, different types of modifications have been carried out on this prototype compound. These include substitution of the ethoxy group at the C-400 position by alkoxy groups of different length, branching, conformational freedom or functionalization. In addition, the 400-ethoxy group has been removed or substituted by other functional groups. The role of the tert-butyldimethylsilyl (TBDMS) group at the 20 position has also been studied by preparing the corresponding 20-deprotected derivative or by replacing it by other silyl (terthexyldimethylsilyl) or acyl (acetyl) moieties. Finally, the thymine of the prototype compound has been replaced by N-3-methylthymine, uracil or thiophenyl. Some of these compounds were endowed with a 6- to 7-fold higher selectivity than the prototype 1. The tricyclic nucleosides here described represent a novel type of selective anti HIV-1 inhibitors, targeted at the HIV-1-encoded reverse transcriptase.
Publisher version (URL)http://dx.doi.org/10.1016/j.antiviral.2011.05.002
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