Discovery of 3,5-disubstituted-1H

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• 作者：Samarjit Patnaik ; Kirk L. Stevens ; Roseanne Gerding ; Felix De ; a ; J. Brad Shotwell ; Jun Tang ; Toshihiro Hamajima ; Hiroko Nakamura ; M. Anthony Leesnitzer ; Anne M. Hassell ; Lisa M. Shewchuck ; Rakesh Kuma
• 关键词：IGF-1R ; IGF-IR ; Pyrrolopyridine ; Kinase inhibitor
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2009
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 June 2009
• 卷：19
• 期：11
• 页码：3136-3140
• 文件大小：2638 K

摘要

Exploration of the SAR around a series of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines led to the discovery of novel pyrrolopyridine inhibitors of the IGF-1R tyrosine kinase. Several compounds demonstrated nanomolar potency in enzyme and cellular mechanistic assays.