| Literature DB >> 22801646 |
John Liddle1, Paul Bamborough, Michael D Barker, Sebastien Campos, Chun-Wa Chung, Rick P C Cousins, Paul Faulder, Michelle L Heathcote, Heather Hobbs, Duncan S Holmes, Chris Ioannou, Cesar Ramirez-Molina, Mary A Morse, Ruth Osborn, Jeremy J Payne, John M Pritchard, William L Rumsey, Daniel T Tape, Giorgia Vicentini, Caroline Whitworth, Rick A Williamson.
Abstract
The lead optimization of a series of potent azaindole IKK2 inhibitors is described. Optimization of the human whole blood activity and selectivity over IKK1 in parallel led to the discovery of 16, a potent and selective IKK2 inhibitor showing good efficacy in a rat model of neutrophil activation.Entities:
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Year: 2012 PMID： 22801646 DOI： 10.1016/j.bmcl.2012.06.065
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823