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.
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https://hal.archives-ouvertes.fr/hal-02086014
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Submitted on : Monday, April 1, 2019 - 9:49:25 AM
Last modification on : Thursday, June 20, 2019 - 9:52:06 AM

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Franck Amblard, Vincent Aucagne, Pierre Guenot, Raymond Schinazi, Luigi Agrofoglio. Synthesis and antiviral activity of novel acyclic nucleosides in the 5-alkynyl- and 6-alkylfuro[2,3-d]pyrimidine series. Bioorganic and Medicinal Chemistry, Elsevier, 2005, 13 (4), pp.1239-1248. ⟨10.1016/j.bmc.2004.11.057⟩. ⟨hal-02086014⟩

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