Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors

被引：14

作者：

Choi, Jang-Sik ^{[1
,2
]}

Hwang, Hae-jun ^{[2
]}

Kim, Se-Won ^{[2
]}

Lee, Byung Il ^{[3
]}

Lee, Jaekyoo ^{[4
]}

Song, Ho-Juhn ^{[4
]}

Koh, Jong Sung ^{[4
]}

Kim, Jung-Ho ^{[2
]}

Lee, Phil Ho ^{[1
]}

机构：

[1] Kangwon Natl Univ, Dept Chem, Chunchon 200701, South Korea

[2] Oscotec Inc, Songnam 463400, Gyeonggi Do, South Korea

[3] Natl Canc Ctr, Res Inst, Div Convergence Technol, Biomol Funct Res Branch, Goyang 410769, Gyeonggi, South Korea

[4] Genosco, Cambridge, MA 02138 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2015年 / 25卷 / 20期

基金：

新加坡国家研究基金会;

关键词：

Spleen tyrosine kinase; Pyrazolylpyrimidine; Syk inhibitors; Rheumatoid arthritis; Structure-activity relationship; SPLEEN TYROSINE KINASE; DISCOVERY; INFLAMMATION; ACTIVATION; TARGET;

D O I：

10.1016/j.bmcl.2015.09.011

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of pyrazolylpyrimidine scaffold based Syk inhibitors were synthesized and evaluated for their biological activities and selectivity. Lead optimization efforts provided compounds with potent Syk inhibition in both enzymatic and TNF-a release assay. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：4441 / 4446

页数：6

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