Disubstituted pyrimidines as Lck inhibitors

被引：7

作者：

Hunt, Julianne A. ^{[1
]}

Beresis, Richard T. ^{[1
]}

Goulet, Joung L. ^{[1
]}

Holmes, Mark A. ^{[1
]}

Hong, Xinfang J. ^{[1
]}

Kovacs, Ernest ^{[1
]}

Mills, Sander G. ^{[1
]}

Ruzek, Rowena D. ^{[1
]}

Wong, Frederick ^{[1
]}

Hermes, Jeffrey D. ^{[1
]}

Park, Young-Whan ^{[1
]}

Salowe, Scott P. ^{[1
]}

Sonatore, Lisa M. ^{[1
]}

Wu, Lin ^{[1
]}

Woods, Andrea ^{[1
]}

Zaller, Dennis M. ^{[1
]}

Sinclair, Peter J. ^{[1
]}

机构：

[1] Merck & Co Inc, Merck Res Labs, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 18期

关键词：

Lck; Src; Protein tyrosine kinase; Autoimmune disease; Rheumatoid arthritis; Pyrimidine; VIVO ANTIINFLAMMATORY ACTIVITY; PROTEIN-TYROSINE KINASES; ORALLY-ACTIVE INHIBITORS; DISCOVERY; ANTIGEN; POTENT; SAR;

D O I：

10.1016/j.bmcl.2009.07.102

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have developed a family of 4-benzimidazolyl-N-piperazinethyl-pyrimidin-2-amines that are subnanomolar inhibitors of Lck. A subset of these Lck inhibitors, with heterocyclic substituents at the benzimidazole C5, are also low-nanomolar inhibitors of cellular IL2 release. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：5440 / 5443

页数：4

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