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

被引：48

作者：

Bamborough, Paul

Christopher, John A.

Cutler, Geoffrey J.

Dickson, Marion C.

Mellor, Geoffrey W.

Morey, James V.

Patel, Champa B.

Shewchuk, Lisa M.

机构：

[1] GlaxoSmithKline R&D, Med Res Ctr, Stevenage SG1 2NY, Herts, England

[2] GlaxoSmithKline Res & Dev Ltd, Harlow CM19 5AW, Essex, England

[3] GlaxoSmithKline Inc, Res Triangle Pk, NC 27709 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 24期

关键词：

IKK-epsilon kinase inhibitors; IKK;

D O I：

10.1016/j.bmcl.2006.09.018

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The identification and hit-to-lead exploration of a novel, potent and selective series of substituted benzimidazole-thiophene carbonitrile inhibitors of IKK-epsilon kinase is described. Compound 12e was identified with an IKK-epsilon enzyme potency of pIC(50) 7.4, and has a highly encouraging wider selectivity profile, including selectivity within the IKK kinase family. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：6236 / 6240

页数：5

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