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Bioorg Med Chem Lett
; 23(9): 2585-9, 2013 May 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-23545108
RESUMEN
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.