Discovery of a Potent Boronic Acid Derived Inhibitor of the HCV RNA-Dependent RNA Polymerase

Andrew Maynard, Renae M Crosby, Byron Ellis, Robert Hamatake, Zhi Hong, Brian A Johns, Kirsten M Kahler, Cecilia Koble, Anna L Leivers, Martin R Leivers, Amanda Mathis, Andrew J Peat, Jeffrey J Pouliot, Christopher D Roberts, Vicente Samano, Rachel M Schmidt, Gary K Smith, Andrew Spaltenstein, Eugene L Stewart, Pia ThommesElizabeth M Turner, Christian Voitenleitner, Jill T Walker, Greg Waitt, Jason Weatherhead, Kurt L Weaver, Shawn Williams, Lois Wright, Zhiping Z Xiong, David Haigh, J Brad Shotwell

Research output: Contribution to journalArticlepeer-review

33 Citations (Scopus)


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 sub-genomic 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 GSK5852 (3), a molecule which entered clinical trials in subjects infected with HCV in 2011, is included.
Original languageEnglish
JournalJournal of Medicinal Chemistry
Early online date14 May 2013
Publication statusEarly online date - 14 May 2013

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