Scaffold oriented synthesis part 4: Design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing heterocycle forming and multicomponent reactions

被引：38

作者：

Akritopoulou-Zanze, Irini ^{[1
]}

Wakefield, Brian D. ^{[1
]}

Gasiecki, Alan ^{[1
]}

Kalvin, Douglas ^{[1
]}

Johnson, Eric F. ^{[1
]}

Kovar, Peter ^{[1
]}

Djuric, Stevan W. ^{[1
]}

机构：

[1] Abbott Labs, Global Pharmaceut Res & Dev, Abbott Pk, IL 60044 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 05期

关键词：

Kinase scaffolds; Kinase inhibitors; Gsk3 beta inhibitors; Rock2; inhibitors; Egfr inhibitors; Imidazopyrimidine; Imidazopyridines; Van Leusen reactions; MCR; multicomponent reactions; 3-COMPONENT CONDENSATION; PREDICTION; PYRAZINES;

D O I：

10.1016/j.bmcl.2011.01.001

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report the synthesis and biological evaluation of 5-substituted indazoles as kinase inhibitors. The compounds were synthesized in a parallel synthesis fashion from readily available starting materials employing heterocycle forming and multicomponent reactions and were evaluated against a panel of kinase assays. Potent inhibitors were identified for Gsk3 beta, Rock2, and Egfr. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：1480 / 1483

页数：4

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