(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives:: Further optimisation as highly potent and selective MSK-1-inhibitors

被引：26

作者：

Bamford, MJ ^{[1
]}

Bailey, N ^{[1
]}

Davies, S ^{[1
]}

Dean, DK ^{[1
]}

Francis, L ^{[1
]}

Panchal, TA ^{[1
]}

Parr, CA ^{[1
]}

Sehmi, S ^{[1
]}

Steadman, JG ^{[1
]}

Takle, AK ^{[1
]}

Townsend, JT ^{[1
]}

Wilson, DM ^{[1
]}

机构：

[1] GlaxoSmithKline Pharmaceut, Neurol & GI Ctr Excellence Drug Discovery, Harlow CM19 5AW, Essex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 14期

关键词：

MSK-1; mitogen and stress-activated protein kinase; imidazo[4,5-c]pyridine;

D O I：

10.1016/j.bmcl.2005.05.020

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The novel imidazo[4,5-c]pyridine 1,2,5-oxadiazol-3-yl template affords an excellent start point for identification of inhibitors of a number of protein kinases. Here we report on its optimisation for mitogen and stress-activated protein kinase-1 (MSK-1) inhibitory activity, and selectivity over other kinases. (c) 2005 Published by Elsevier Ltd.

引用

页码：3407 / 3411

页数：5

共 14 条

[1]

BAMFORD MJ, 2005, BIOORG MED CHEM LETT, V15, P3405

[2]

Barone FC, 2001, MED RES REV, V21, P129, DOI 10.1002/1098-1128(200103)21:2<129::AID-MED1003>3.0.CO

[3]

2-H

[4] Specificity and mechanism of action of some commonly used protein kinase inhibitors [J].