Molecular design, synthesis, and structure-activity relationships leading to the potent and selective P56lck inhibitor BMS-243117

被引：61

作者：

Das, J ^{[1
]}

Lin, J ^{[1
]}

Moquin, RV ^{[1
]}

Shen, ZQ ^{[1
]}

Spergel, SH ^{[1
]}

Wityak, J ^{[1
]}

Doweyko, AM ^{[1
]}

DeFex, HF ^{[1
]}

Fang, Q ^{[1
]}

Pang, SH ^{[1
]}

Pitt, S ^{[1
]}

Shen, DR ^{[1
]}

Schieven, GL ^{[1
]}

Barrish, JC ^{[1
]}

机构：

[1] Bristol Myers Squibb Pharmaceut Res Inst, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 13期

关键词：

D O I：

10.1016/S0960-894X(03)00380-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of structurally novel benzothiazole based small molecule inhibitors of p56(lck) were prepared to elucidate their structure-activity relationships (SARs), selectivity and cell activity in the T-cell proliferation assay. BMS-243117 (compound 2) is identified as a potent, and selective Lck inhibitor with good cellular activity (IC50 = 1.1 muM) against T-cell proliferation. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：2145 / 2149

页数：5

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