Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK)

被引：27

作者：

Farmer, Luc J. ^{[1
]}

Bemis, Guy ^{[1
]}

Britt, Shawn D. ^{[1
]}

Cochran, John ^{[1
]}

Connors, Martin ^{[1
]}

Harrington, Edmund M. ^{[1
]}

Hoock, Thomas ^{[1
]}

Markland, William ^{[1
]}

Nanthakumar, Suganthini ^{[1
]}

Taslimi, Paul ^{[1
]}

Ter Haar, Ernst ^{[1
]}

Wang, Jian ^{[1
]}

Zhaveri, Darshana ^{[1
]}

Salituro, Francesco G. ^{[1
]}

机构：

[1] Vertex Pharmaceut Inc, Dept Med Chem, Cambridge, MA 02139 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 23期

关键词：

SYK; Spleen tyrosine kinase; Asthma;

D O I：

10.1016/j.bmcl.2008.09.106

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of SYK inhibitors based on the phenylamino pyrimidine thiazole lead 4 were prepared and evaluated for biological activity. Lead optimization provided compounds with nanomolar K-i's against SYK and potent inhibition in mast cell degranulation assays. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：6231 / 6235

页数：5

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