Design and effective synthesis of novel templates, 3,7-diphenyl-4amino-thieno and furo-[3,2-c]pyridines as protein kinase inhibitors and in vitro evaluation targeting angiogenetic kinases
Design and effective synthesis of novel templates, 3,7-diphenyl-4amino-thieno and furo-[3,2-c]pyridines as protein kinase inhibitors and in vitro evaluation targeting angiogenetic kinases
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DOI：
10.1016/j.bmcl.2006.09.050
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发表时间：
2007-01-01
影响因子：
2.7
通讯作者：
Kane-Carson, Laurie
中科院分区：
文献类型：
--
作者：
Miyazaki, Yasushi;Nakano, Masato;Kane-Carson, Laurie
基于 ATP 竞争性激酶抑制剂的药效团模型，设计了一类新型 3,7-二苯基-4-氨基噻吩和呋喃[3,2-c]吡啶。已经建立了通过双 Suzuki 偶联探索 SAR 的多功能合成方法，并成功发现了针对血管生成靶点 VEGFR2、Tie-2 和 EphB4 的有效抑制剂。 (c) 2006 Elsevier Ltd. 保留所有权利。
A novel class of 3,7-diphenyl-4-amino-thieno and furo[3,2-c]pyridine has been designed based on pharmacophore models of ATP competitive kinase inhibitors. Versatile synthetic methods via double Suzuki coupling to explore SAR have been established and potent inhibitors against angiogenetic targets, VEGFR2, Tie-2, and EphB4, have been successfully discovered. (c) 2006 Elsevier Ltd. All rights reserved.