A novel 2',3'-dideoxy-2'-α-fluoro-2'-β--methyl-6-methoxy guanosine () and its phosphoramidate prodrug () 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 μM) in the Huh-7 cell line. The prodrug () displayed nanomolar level antiviral activity (EC = 0.39-1.1 μM) against the HCV genotype (GT) 1a, 1b, 2a, and 1b S282T replicons.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5467188 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.7b00174 | DOI Listing |
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