Structure-activity relationships of a novel class of Src SH2 inhibitors

被引:52
作者
Buchanan, JL [1 ]
Vu, CB [1 ]
Merry, TJ [1 ]
Corpuz, EG [1 ]
Pradeepan, SG [1 ]
Mani, UN [1 ]
Yang, M [1 ]
Plake, HR [1 ]
Varkhedkar, VM [1 ]
Lynch, BA [1 ]
MacNeil, IA [1 ]
Loiacono, KA [1 ]
Tiong, CL [1 ]
Holt, DA [1 ]
机构
[1] ARIAD Pharmaceut Inc, Cambridge, MA 02139 USA
关键词
D O I
10.1016/S0960-894X(99)00389-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The structure-activity relationships (SAR) of a novel class of Src SH2 inhibitors are described. Variation at the pY+1 and pY+3 side chain positions using 2,4- and 2,5-substituted thiazoles and 1,2,4-oxadiazoles as scaffolds resulted in inhibitors that bound as well as the standard tetrapeptide Ac-pYEEI-NH2. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2359 / 2364
页数:6
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