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


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.

SUBMITTER: Zhou L 

PROVIDER: S-EPMC4716611 | biostudies-literature | 2016 Jan

REPOSITORIES: biostudies-literature

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

Zhou Longhu L   Zhang Hongwang H   Tao Sijia S   Ehteshami Maryam M   Cho Jong Hyun JH   McBrayer Tamara R TR   Tharnish Philip P   Whitaker Tony T   Amblard Franck F   Coats Steven J SJ   Schinazi Raymond F RF  

ACS medicinal chemistry letters 20151123 1


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. ...[more]

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