Novel imidazo[1,2-a]pyridine based inhibitors of the IGF-1 receptor tyrosine kinase: Optimization of the aniline

被引：37

作者：

Ducray, Richard ^{[1
]}

Jones, Clifford D. ^{[1
]}

Jung, Frederic H. ^{[1
]}

Simpson, Iain ^{[2
]}

Curwen, Jon ^{[2
]}

Pass, Martin ^{[2
]}

机构：

[1] AstraZeneca, Oncol Innovat Med, Ctr Rech, ZI Pompelle, F-51689 Reims 2, France

[2] AstraZeneca, Oncol Innovat Med, Macclesfield SK10 4TG, Cheshire, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 16期

关键词：

IGF1-R; Insulin-like growth factor-1 receptor; Kinase inhibitor; GROWTH-FACTOR RECEPTOR; I RECEPTOR; ONCOLOGY;

D O I：

10.1016/j.bmcl.2011.06.090

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

Following the discovery of imidazopyridine 1 as a potent IGF-1R tyrosine kinase inhibitor, the aniline part has been modified with the aim to optimize the properties of this series. The structure-activity relationships against IGF-1R kinase activity as well as inhibition of the hERG ion channel are discussed. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：4702 / 4704

页数：3

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