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Amblard, F ; Aucagne, V ; Guenot, P ; Schinazi, RF ; Agrofoglio, LA

Synthesis and antiviral activity of novel acyclic nucleosides in the 5-alkynyl- and 6-alkylfuro[2,3-d]pyrimidine series

Bioorganic & Medicinal Chemistry 13 (4) 1239-1248

par Administrateur - publié le

Abstract :

The synthesis of novel acyclic nucleosides in the 5-alkynyl and 6-alkylfuro[2,3-d]pyrimidine series is described. These compounds were evaluated against HIV and HSV in order to determine their spectrum of antiviral activity. Their cytotoxicities against PBM, CEM and VERO cells were also determined. Compounds 21d and 24b displayed moderate EC50S of 2.7 and 4.9 muM, respectively, against HIV-1 and of 6.3 and 4.8 muM, respectively, against HSV. Nevertheless, these compounds also showed cellular toxicity, suggesting that the antiviral effects are secondary to the toxic effects. (C) 2004 Elsevier Ltd. All rights reserved.