Using a cell-based replicon screen, we identified a class of compounds with a thiazolidinone
core structure as inhibitors of hepatitis C virus (HCV) replication. The concentration of one …

The iminothiazolidinone BMS-858 (2) was identified as a specific inhibitor of HCV replication
in a genotype 1b replicon assay via a high-throughput screening campaign. A more potent …

The biphenyl derivatives 2 and 3 are prototypes of a novel class of NS5A replication complex
inhibitors that demonstrate high inhibitory potency toward a panel of clinically relevant …

Lead inhibitors that target the function of the hepatitis C virus (HCV) nonstructural 5A (NS5A)
protein have been identified by phenotypic screening campaigns using HCV subgenomic …

The synthesis and biological activity of sordarin oxazepine derivatives are described. The
key step features a regioselective oxidation of an unprotected triol followed by double …

Cyclization of unsymmetrical thioureas affords 3-(heteroaryl)-iminothiazolidin-4-ones with
excellent levels of regiocontrol. In the absence of base, 2-(pyridylmethyl) and 2-(aminomethyl)…

Methods for selectively protecting one of the degenerate nitrogen atoms of the cyclic urea
derivatives 1.3-dihydro-2H-benzimidazol-2-one (6a), l, 3-dihydro-2H-imidazo [4, 5-f>] pyridin-2-…

The hepatitis C virus NS5A protein is an established and clinically validated target for antiviral
intervention by small molecules. Characterizations are presented of compounds identified …

A series of symmetrical E-stilbene prolinamides that originated from the library-synthesized
lead 3 was studied with respect to HCV genotype 1a (G-1a) and genotype 1b (G-1b) replicon …

A series of fluoroglycosylated fluoroindolocarbazoles was examined with respect to their
topoisomerase I activity, cytotoxicity, and selectivity. The lead clinical candidate from this series, …