Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors.: Part 2

被引：50

作者：

Choi, HS

Wang, ZC

Richmond, W

He, XH

Yanga, KY

Jiang, T

Karanewsky, D

Gu, XJ

Zhou, V

Liu, Y

Che, JW

Lee, CC

Caldwell, J

Kanazawa, T

Umemura, I

Matsuura, N

Ohmori, O

Honda, T

Gray, N

He, Y

机构：

[1] Novartis Res Fdn GNF, Genom Inst, San Diego, CA 92138 USA

[2] Novartis Inst BioMed Res Tsukuba, Tsukuba, Ibaraki 3002611, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 10期

关键词：

7H-pyrrolo[2,3-d]pyrimidines; focal adhesion kinase (FAK); molecular modeling; SAR; kinase inhibitor;

D O I：

10.1016/j.bmcl.2006.02.032

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2-amino-9-aryl-7H-pyrrolo[2,3-d] pyrimidines were designed and synthesized as focal adhesion kinase (FAK) inhibitors using molecular modeling in conjunction with a co-crystal structure. Chemistry was developed to introduce functionality onto the 9-aryl ring, which resulted in the identification of potent FAK inhibitors. In particular, compound 32 possessed single-digit nanomolar IC50 and represents one of the most potent FAK inhibitors discovered to date. (C) 2006 Elsevier Ltd. All rights reserved.

引用

页码：2689 / 2692

页数：4

共 12 条

[1] SYNTHESIS AND PROPERTIES OF HALOHYDROXYACETONES AND HALOMETHYLGLYOXALS [J].