Synthesis and SAR of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors

被引：23

作者：

Shin, Youseung

Chen, Weiming

Habel, Jeff

Duckett, Derek

Ling, Yuan Yuan

Koenig, Marcel

He, Yuanjun

Vojkovsky, Tomas

LoGrasso, Philip ^{[1
]}

Kamenecka, Theodore M.

机构：

[1] Scripps Res Inst, Dept Mol Therapeut, Jupiter, FL 33458 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 12期

关键词：

JNK; Kinase; ACTIVATED PROTEIN-KINASES; SELECTIVE INHIBITORS; DESIGN; POTENT; INFLAMMATION; APOPTOSIS; ASTHMA;

D O I：

10.1016/j.bmcl.2009.03.086

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of c-jun N-terminal kinase (JNK) inhibitors were designed and developed from a high-throughput-screening hit. Through the optimization of the piperazine amide 1, several potent compounds were discovered. The X-ray crystal structure of 4g showed a unique binding mode different from other well known JNK3 inhibitors. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：3344 / 3347

页数：4

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