Synthesis and Evaluation of 2,6-Modified Purine 2'-C-Methyl Ribonucleosides as Inhibitors of HCV Replication

ACS Med Chem Lett. 2015 Nov 23;7(1):17-22. doi: 10.1021/acsmedchemlett.5b00402. eCollection 2016 Jan 14.

Abstract

A variety of 2,6-modified purine 2'-C-methylribonucleosides and their phosphoramidate prodrugs were synthesized and evaluated for inhibition of HCV RNA replication in Huh-7 cells and for cytotoxicity in various cell lines. Cellular pharmacology and HCV polymerase incorporation studies on the most potent and selective compound are reported.

Keywords: HCV; antiviral; nucleoside; phosphoramidate prodrug; purine.