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4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors
Authors:John Liddle  Paul Bamborough  Michael D Barker  Sebastien Campos  Rick PC Cousins  Geoffrey J Cutler  Heather Hobbs  Duncan S Holmes  Chris Ioannou  Geoff W Mellor  Mary A Morse  Jeremy J Payne  John M Pritchard  Kathryn J Smith  Daniel T Tape  Caroline Whitworth  Richard A Williamson
Institution:1. GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, UK;2. GlaxoSmithKline R&D, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
Abstract: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.
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