Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase

被引：25

作者：

Patnaik, Samarjit ^{[1
]}

Stevens, Kirk L. ^{[1
]}

Gerding, Roseanne ^{[1
]}

Deanda, Felix ^{[2
]}

Shotwell, J. Brad ^{[1
]}

Tang, Jun ^{[1
]}

Hamajima, Toshihiro ^{[3
]}

Nakamura, Hiroko ^{[3
]}

Leesnitzer, M. Anthony ^{[1
]}

Hassell, Anne M. ^{[1
]}

Shewchuck, Lisa M. ^{[2
]}

Kumar, Rakesh ^{[4
]}

Lei, Huangshu ^{[1
]}

Chamberlain, Stanley D. ^{[1
]}

机构：

[1] GlaxoSmithKline, Oncol R&D, Res Triangle Pk, NC 27709 USA

[2] GlaxoSmithKline, Computat & Struct Chem, Res Triangle Pk, NC 27709 USA

[3] GlaxoSmithKline, K K Tsukuba Res Labs, Ibaraki 3004247, Japan

[4] GlaxoSmithKline, Oncol R&D, Collegeville, PA 19426 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 11期

关键词：

IGF-1R; IGF-IR; Pyrrolopyridine; Kinase inhibitor; SELECTIVE INHIBITOR; CANCER; VIVO;

D O I：

10.1016/j.bmcl.2008.12.110

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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. (C) 2009 Published by Elsevier Ltd.

引用

页码：3136 / 3140

页数：5

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