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Discovery of pyrano[3,4-b]indoles as potent and selective HCV NS5B polymerase inhibitors.

Journal of medicinal chemistry 2004 Dec 16; 47(26):6603-8

Link to PubMed abstract

Gopalsamy A A, Lim K K, Ciszewski G G, Park K K, Ellingboe J JW, Bloom J J, Insaf S S, Upeslacis J J, Mansour T TS, Krishnamurthy G G, Damarla M M, Pyatski Y Y, Ho D D, Howe A AY, Orlowski M M, Feld B B, O'Connell J J

Chemical and Screening Sciences and Infectious Diseases, Wyeth Research, Pearl River, New York 10965, USA. gopalsa@wyeth.com

A novel series of HCV NS5B RNA-dependent RNA polymerase inhibitors containing a pyrano[3,4-b]indole scaffold is described leading to the discovery of compound 16, a highly potent and selective inhibitor that is active in the replicon system.