title: Synthesis and antiviral activity of novel acyclic nucleosides in the 5-alkynyl- and 6-alkylfuro[2,3-d]pyrimidine series.
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 microM, respectively, against HIV-1 and of 6.3 and 4.8 microM, respectively, against HSV. Nevertheless, these compounds also showed cellular toxicity, suggesting that the antiviral effects are secondary to the toxic effects.
authors.affiliation: Institut de Chimie Organique et Analytique, ICOA UMR 6005, UFR Sciences, BP 6759, 45067 Orléans Cedex 2, France.
authors.forename: Franck
authors.initials: F
authors.lastname: Amblard
authors.forename: Vincent
authors.initials: V
authors.lastname: Aucagne
authors.forename: Pierre
authors.initials: P
authors.lastname: Guenot
authors.forename: Raymond F
authors.initials: RF
authors.lastname: Schinazi
authors.forename: Luigi A
authors.initials: LA
authors.lastname: Agrofoglio
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002460:Cell Line; D006678:HIV / Q000187:drug effects; D006801:Humans; D013058:Mass Spectrometry; D008826:Microbial Sensitivity Tests; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D018139:Simplexvirus / Q000187:drug effects
chemical_list: D000998:Antiviral Agents; D011743:Pyrimidines