4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors

J Liddle, P Bamborough, MD Barker, S Campos…

Index: Liddle, John; Bamborough, Paul; Barker, Michael D.; Campos, Sebastien; Cousins, Rick P.C.; Cutler, Geoffrey J.; Hobbs, Heather; Holmes, Duncan S.; Ioannou, Chris; Mellor, Geoff W.; Morse, Mary A.; Payne, Jeremy J.; Pritchard, John M.; Smith, Kathryn J.; Tape, Daniel T.; Whitworth, Caroline; Williamson, Richard A. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 9 p. 2504 - 2508

Full Text: HTML

Citation Number: 25

Abstract

Download PDF Opens in a new window. Article suggestions will be shown in a dialog on return to ScienceDirect. ... Please enable JavaScript to use all the features on this page. ... The synthesis and SAR of a novel series of IKK2 inhibitors are described. Modification around the hinge binding region of the 7-azaindole led to a series of potent and selective inhibitors with good cellular activity. ... The synthesis and SAR of 4-aryl-7-azaindoles as ATP-competitive IKK2 ...