Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors

被引：54

作者：

Terao, Yoshito ^{[1
]}

Suzuki, Hideo ^{[1
]}

Yoshikawa, Masato ^{[1
]}

Yashiro, Hiroaki ^{[1
]}

Takekawa, Shiro ^{[1
]}

Fujitani, Yasushi ^{[1
]}

Okada, Kengo ^{[1
]}

Inoue, Yoshihisa ^{[1
]}

Yamamoto, Yoshio ^{[1
]}

Nakagawa, Hideyuki ^{[1
]}

Yao, Shuhei ^{[1
]}

Kawamoto, Tomohiro ^{[1
]}

Uchikawa, Osamu ^{[1
]}

机构：

[1] Takeda Pharmaceut Co Ltd, Div Pharmaceut Res, Fujisawa, Kanagawa 2518555, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 24期

关键词：

ASK1; Imidazo[1,2-a]pyridine; LLE; SIGNALING PATHWAYS; APOPTOSIS; APOPTOSIS-SIGNAL-REGULATING-KINASE-1; IDENTIFICATION;

D O I：

10.1016/j.bmcl.2012.10.084

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Imidazo[1,2-a]pyridine derivatives were designed, synthesized, and evaluated as inhibitors of the apoptosis signal-regulating kinase 1 (ASK1). These were based on a benzothiazole derivative that was discovered from high-throughput screening of our compound library. As a result, we identified potent, selective, and orally bioavailable ASK1 inhibitors for wide range of therapeutic targets. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：7326 / 7329

页数：4

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