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

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• 作者：Paul Bamborough ; John A. Christopher ; Geoffrey J. Cutler ; Marion C. Dickson ; Geoffrey W. Mellor ; James V. Morey ; Champa B. Patel ; Lisa M. Shewchuk
• 关键词：IKK-ε ; kinase inhibitors ; IKK
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：15 December 2006
• 年：2006
• 卷：16
• 期：24
• 页码：6236-6240
• 全文大小：286 K

文摘

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.