Aminopyridine carboxamides as c-Jun N-terminal kinase inhibitors: Targeting the gatekeeper residue and beyond

被引：21

作者：

Liu, Gang ^{[1
]}

Zhao, Hongyu ^{[1
]}

Liu, Bo ^{[1
]}

Xin, Zhili ^{[1
]}

Liu, Mei ^{[1
]}

Kosogof, Christi ^{[1
]}

Szczepankiewicz, Bruce G. ^{[1
]}

Wang, Sanyi ^{[1
]}

Clampit, Jill E. ^{[1
]}

Gum, Rebecca J. ^{[1
]}

Haasch, Deanna L. ^{[1
]}

Trevillyan, James M. ^{[1
]}

Sham, Hing L. ^{[1
]}

机构：

[1] Abbott Labs, Metab Dis Res, Global Pharmaceut Res & Dev, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 22期

关键词：

JNK inhibitors; gatekeeper residue; specificity pocket; ribose pocket;

D O I：

10.1016/j.bmcl.2006.08.097

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The structure-activity relationships of 5,6-positions of aminopyridine carboxamide-based c-Jun N-terminal Kinase (JNK) inhibitors were explored to expand interaction with the kinase specificity and ribose-binding pockets. The syntheses of analogues and the impact of structural modification on in vitro potency and cellular activity are described. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：5723 / 5730

页数：8

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