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
收藏
页码：3344 / 3347
页数：4
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