1331942-27-8Relevant articles and documents
Discovery of a potent boronic acid derived inhibitor of the HCV RNA-dependent RNA polymerase
Maynard, Andrew,Crosby, Renae M.,Ellis, Byron,Hamatake, Robert,Hong, Zhi,Johns, Brian A.,Kahler, Kirsten M.,Koble, Cecilia,Leivers, Anna,Leivers, Martin R.,Mathis, Amanda,Peat, Andrew J.,Pouliot, Jeffrey J.,Roberts, Christopher D.,Samano, Vicente,Schmidt, Rachel M.,Smith, Gary K.,Spaltenstein, Andrew,Stewart, Eugene L.,Thommes, Pia,Turner, Elizabeth M.,Voitenleitner, Christian,Walker, Jill T.,Waitt, Greg,Weatherhead, Jason,Weaver, Kurt,Williams, Shawn,Wright, Lois,Xiong, Zhiping Z.,Haigh, David,Shotwell, J. Brad
, p. 1902 - 1913 (2014/04/03)
A boronic acid moiety was found to be a critical pharmacophore for enhanced in vitro potency against wild-type hepatitis C replicons and known clinical polymorphic and resistant HCV mutant replicons. The synthesis, optimization, and structure-activity relationships associated with inhibition of HCV replication in a subgenomic replication system for a series of non-nucleoside boron-containing HCV RNA-dependent RNA polymerase (NS5B) inhibitors are described. A summary of the discovery of 3 (GSK5852), a molecule which entered clinical trials in subjects infected with HCV in 2011, is included.
