Synthesis and SAR of 4-(pyrazol-3-yl)-pyridines as novel c-jun N-terminal kinase inhibitors

被引：17

作者：

Noel, Romain ^{[1
]}

Shin, Youseung ^{[1
]}

Song, Xinyi ^{[1
]}

He, Yuanjun ^{[1
]}

Koenig, Marcel ^{[1
]}

Chen, Weimin ^{[1
]}

Ling, Yuan Yuan ^{[1
]}

Lin, Li ^{[1
]}

Ruiz, Claudia H. ^{[1
]}

LoGrasso, Phil ^{[1
]}

Cameron, Michael D. ^{[1
]}

Duckett, Derek R. ^{[1
]}

Kamenecka, Theodore M. ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 09期

关键词：

JNK; Kinase; c-Jun; ACTIVATED PROTEIN-KINASES; JNK INHIBITORS; SELECTIVE INHIBITORS; DESIGN; POTENT; INFLAMMATION; APOPTOSIS; PATHWAYS; SCAFFOLD; ASTHMA;

D O I：

10.1016/j.bmcl.2010.11.104

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The design and synthesis of a novel series of c-jun N-terminal kinase (JNK) inhibitors is described. The development of the 4-(pyrazol-3-yl)-pyridine series was discovered from an earlier pyrimidine series of JNK inhibitors. Through the optimization of the scaffold 2, several potent compounds with good in vivo profiles were discovered. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：2732 / 2735

页数：4

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