Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56lck inhibitors

被引：108

作者：

Das, J ^{[1
]}

Moquin, RV ^{[1
]}

Lin, J ^{[1
]}

Liu, CJ ^{[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
]}

Wityak, J ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 15期

关键词：

D O I：

10.1016/S0960-894X(03)00511-0

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) was prepared to elucidate their structure-activity relationships (SAR), selectivity and cell activity in the T-cell proliferation assay. BMS-350751 (2) and BMS-358233 (3) are identified as potent Lck inhibitors with excellent cellular activities against T-cell proliferation. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：2587 / 2590

页数：4

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