1313201-84-1Relevant articles and documents
Synthesis and anti-HIV evaluation of 3′-triazolo nucleosides
Roy, Vincent,Obikhod, Aleksandr,Zhang, Hong-Wang,Coats, Steven J.,Herman, Brian D.,Sluis-Cremer, Nicolas,Agrofoglio, Luigi A.,Schinazi, Raymond F.
, p. 264 - 270 (2012/02/03)
A series of hitherto unknown 3′-α-[1,2,3]-substituted triazolo-2′,3′-dideoxypyrimidine nucleoside analogues of the anti-HIV 3′-azido-3′-deoxythymidine (AZT) were synthesized through catalyzed alkyne-azide 1,3-dipolar cycloaddition (Huisgen reaction). Those 3′-[1,2,3]-triazolo analogues bearing an azido alkyl chain were evaluated for their anti-HIV activity against HIV-1 in primary human lymphocytes as well as for their cytotoxicity in different cells. None of them inhibit HIV replication (EC50 > 20 μM); two of them were converted to their triphosphate form to evaluate their HIV-RT inhibition. Copyright Taylor and Francis Group, LLC.
