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

F Amblard, V Aucagne, P Guenot, RF Schinazi…

Index: Amblard, Franck; Aucagne, Vincent; Guenot, Pierre; Schinazi, Raymond F.; Agrofoglio, Luigi A. Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 4 p. 1239 - 1248

Full Text: HTML

Citation Number: 52

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 μM, respectively, against HIV-1 and of 6.3 and 4.8 μM, respectively, against ...