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Synthesis and anti-HCV activity of a new 2′-deoxy-2′-fluoro-2′-C-methyl nucleoside analogue

✍ Scribed by Weidong Hu; Ping’an Wang; Chuanjun Song; Zhenliang Pan; Qiang Wang; Xiaohe Guo; Xuejun Yu; Zhenhua Shen; Shuyang Wang; Junbiao Chang


Publisher
Elsevier Science
Year
2010
Tongue
English
Weight
260 KB
Volume
20
Category
Article
ISSN
0960-894X

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✦ Synopsis


2 0 -Deoxy-2 0 -fluoro-2 0 -C-methyl nucleoside Anti-HCV activity a b s t r a c t 2 0 -Deoxy-2 0 -fluoro-2 0 -C-methyl nucleoside analogue 4 was designed and synthesized. Initial biological studies indicated that this compound showed promising activity against HCV replication.


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Based on the favorable antiviral profiles of 4'-substituted nucleosides, novel 1-(2'-deoxy-2'-fluoro-4'-C-ethynyl-beta-D-arabinofuranosyl)-uracil (1a), -thymine (1b), and -cytosine (2) analogs were synthesized. Compounds 1b and 2 exhibited potent anti-HIV-1 activity with IC(50) values of 86 and 1.34