Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56Lck inhibitors

被引:34
|
作者
Ping, C
Norris, D
Das, J
Spergel, SH
Wityak, J
Leith, L
Zhao, RL
Chen, BC
Pitt, S
Pang, SH
Ding, RS
Zhang, R
De Fex, HF
Doweyko, AM
McIntyre, KW
Shuster, DJ
Behnia, K
Schieven, GL
Barrish, JC
机构
[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Discovery Chem, Princeton, NJ 08543 USA
[2] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Immunol Inflammat & Pulm Drug Discovery, Princeton, NJ 08543 USA
[3] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Macromol Sci, Princeton, NJ 08543 USA
[4] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Metab & Pharmacokinet, Princeton, NJ 08543 USA
关键词
Lck inhibitor; pan-Src-family inhibitor;
D O I
10.1016/j.bmcl.2004.09.093
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of substituted 2-(aminoheteroaryl)-thiazole-5-carboxamide analogs have been synthesized as novel, potent inhibitors of the Src-family kinase p56(Lck). Among them, compound 2 displayed superior in vitro potency and excellent in vivo efficacy. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:6061 / 6066
页数:6
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