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. 2012 Aug 15;22(16):5222-6.
doi: 10.1016/j.bmcl.2012.06.065. Epub 2012 Jun 26.

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

John Liddle  1 , 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
Affiliations

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

John Liddle et al. Bioorg Med Chem Lett. .

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.

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