The discovery and structure-activity relationships of pyrano[3,4-b]indole based inhibitors of hepatitis C virus NS5B polymerase

  • Bioorg Med Chem Lett. 2010 May 1;20(9):2968-73. doi: 10.1016/j.bmcl.2010.03.002.
Matthew G LaPorte  1 ,  Tandy L Draper ,  Lori E Miller ,  Charles W Blackledge ,  Lara K Leister ,  Eugene Amparo ,  Alison R Hussey ,  Dorothy C Young ,  Srinivas K Chunduru ,  Christopher A Benetatos ,  Gerry Rhodes ,  Ariamala Gopalsamy ,  Torsten Herbertz ,  Christopher J Burns ,  Stephen M Condon
Affiliations
  • 1. University of Pittsburgh, Center for Chemical Methodologies and Library Development, Pittsburgh, PA 15260, USA. [email protected]
PMID: 20347591 DOI: 10.1016/j.bmcl.2010.03.002
Abstract

We describe the structure-activity relationship of the C1-group of pyrano[3,4-b]indole based inhibitors of HCV NS5B polymerase. Further exploration of the allosteric binding site led to the discovery of the significantly more potent compound 12.