5-(1H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-ε kinase

P Bamborough, JA Christopher, GJ Cutler…

Index: Bamborough, Paul; Christopher, John A.; Cutler, Geoffrey J.; Dickson, Marion C.; Mellor, Geoffrey W.; Morey, James V.; Patel, Champa B.; Shewchuk, Lisa M. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 24 p. 6236 - 6240

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Citation Number: 28

Abstract

The identification and hit-to-lead exploration of a novel, potent and selective series of substituted benzimidazole–thiophene carbonitrile inhibitors of IKK-ε kinase is described. Compound 12e was identified with an IKK-ε enzyme potency of pIC50 7.4, and has a highly encouraging wider selectivity profile, including selectivity within the IKK kinase family.