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

被引：57
|
作者：
Amblard, F
Aucagne, V
Guenot, P
Schinazi, RF
Agrofoglio, LA
机构：
[1] ICOA, UMR 6005, UFR Sci, Inst Chim Organ & Analyt, F-45067 Orleans 2, France
[2] Univ Rennes 1, CRMPO, F-35042 Rennes, France
[3] Emory Univ, Biochem Pharmacol Lab, Dept Pediat, Sch Med, Atlanta, GA 30033 USA
[4] Emory Univ, Sch Med, Vet Affairs Med Ctr, Atlanta, GA 30033 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2005年 / 13卷 / 04期
基金：
美国国家科学基金会;
关键词：
nucleosides; furopyrimidine; antiviral activity;
D O I：
10.1016/j.bmc.2004.11.057
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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.
引用
收藏
页码：1239 / 1248
页数：10
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