Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors
Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors
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DOI：
10.1016/j.bmcl.2008.12.011
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发表时间：
2009-02-01
影响因子：
2.7
通讯作者：
Uehling, David E.
中科院分区：
文献类型：
--
作者：
Rheault, Tara R.;Caferro, Thomas R.;Uehling, David E.
已经鉴定了两个新系列的源自新型噻吩并嘧啶核的强效和选择性双重EGFR/ErbB-2激酶抑制剂。异构体噻吩并嘧啶核被评价为4-苯胺基喹唑啉核的电子等排体，并且含有噻吩并[3，2-d]嘧啶核的几种类似物显示出体外抗人肿瘤细胞的IC 50值小于1 μ M的抗增殖活性。(C)2008爱思唯尔有限公司版权所有。
Two new series of potent and selective dual EGFR/ErbB-2 kinase inhibitors derived from novel thienopyrimidine cores have been identified. Isomeric thienopyrimidine cores were evaluated as isosteres for a 4-anilinoquinazoline core and several analogs containing the thieno[3,2-d]pyrimidine core showed anti-proliferative activity with IC50 values less than 1 mu M against human tumor cells in vitro. (C) 2008 Elsevier Ltd. All rights reserved.