Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371252 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
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.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
John Liddle, 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,