4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy

…, DS Holmes, C Ioannou, C Ramirez-Molina…

Index: Liddle, John; Bamborough, Paul; Barker, Michael D.; Campos, Sebastien; Chung, Chun-Wa; Cousins, Rick P.C.; Faulder, Paul; Heathcote, Michelle L.; Hobbs, Heather; Holmes, Duncan S.; Ioannou, Chris; Ramirez-Molina, Cesar; Morse, Mary A.; Osborn, Ruth; Payne, Jeremy J.; Pritchard, John M.; Rumsey, William L.; Tape, Daniel T.; Vicentini, Giorgia; Whitworth, Caroline; Williamson, Rick A. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 16 p. 5222 - 5226

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Citation Number: 9

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.