| Literature DB >> 23545108 |
Timothy A Stammers1, René Coulombe, Jean Rancourt, Bounkham Thavonekham, Gulrez Fazal, Sylvie Goulet, Araz Jakalian, Dominic Wernic, Youla Tsantrizos, Marc-André Poupart, Michael Bös, Ginette McKercher, Louise Thauvette, George Kukolj, Pierre L Beaulieu.
Abstract
A novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors were derived from a fragment-based approach using information from X-ray crystallographic analysis of NS5B-inhibitor complexes and iterative rounds of parallel synthesis. Structure-based drug design strategies led to the discovery of potent sub-micromolar inhibitors 11a-c and 12a-c from a weak-binding fragment-like structure 1 as a starting point.Entities:
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Year: 2013 PMID： 23545108 DOI： 10.1016/j.bmcl.2013.02.110
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823