Article
Identification and biological evaluation of a series of 1H-benzo[de]isoquinoline-1,3(2H)-diones as hepatitis C virus NS5B polymerase inhibitors.
Journal of medicinal chemistry - 27 Aug 2009
Ontoria Jesus M, Rydberg Edwin H, Di Marco Stefania, Tomei Licia, Attenni Barbara, Malancona Savina, Martin Hernando José I, Gennari Nadia, Koch Uwe, Narjes Frank, Rowley Michael, Summa Vincenzo, Carroll Steve S, Olsen David B, De Francesco Raffaele, Altamura Sergio, Migliaccio Giovanni, Carfì Andrea
Abstract excerpt
The hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) plays a central role in virus replication. NS5B has no functional equivalent in mammalian cells and, as a consequence, is an attractive target for inhibition. Herein, we present 1H-benzo[de]isoquinoline-1,3(2H)-diones as a new series of selective inhibitors of HCV NS5B polymerase. The HTS hit 1 shows submicromolar potency in two different HCV...
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