Synthesis And Anti-Hcv Activity Of A Novel 2,' 3 '-Dideoxy-2 '-Alpha-Fluoro-2 '-Beta-C-Methyl Guanosine Phosphoramidate Prodrug
ACS medicinal chemistry letters(2017)
Abstract
A novel 2',3'-dideoxy-2'-alpha-fluoro-2'-beta-C-methyl-6-methoxy guanosine (8) and its phosphoramidate prodrug (1) have been designed and synthesized. Their biological activity was evaluated in both cytotoxicity and cell-based HCV replicon assays. Neither compounds exhibited cytotoxicity up to the highest concentration tested (100 mu M) in the Huh-7 cell line. The prodrug (1) displayed nanomolar level antiviral activity (EC50 = 0.39-1.1 mu M) against the HCV genotype (GT) la, lb, 2a, and lb S282T replicons.
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Key words
2 ',3 '-Dideoxy guanosine, 2 '-alpha-fluoro-2 '-beta-C-methyl, phosphoramidate prodrug, anti-HCV activity, NSSB RdRp inhibitor
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