☆ 4.5 Article

Discovery and optimization of imidazo[1,2-α]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R)

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2009)

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Volume 19, Issue 3, Pages 1004-1008

Publisher

PERGAMON-ELSEVIER SCIENCE LTD

DOI: 10.1016/j.bmcl.2008.11.058

Keywords

Insulin-like growth factor-1 receptor; Insulin receptor; Kinase inhibitor; Cancer; Imidazo[1,2-a]pyridine

Categories

Chemistry, Medicinal Chemistry, Organic

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Abstract

The optimization of imidazo[1,2-a] pyridine inhibitors as potent and selective inhibitors of IGF-1R is presented. Further optimization of oral exposure in mice is also discussed. Detailed selectivity, in vitro activity, and in vivo PK profiles of an optimized compound is also highlighted. (C) 2008 Elsevier Ltd. All rights reserved.

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