基于噻吩嘧啶的双重 EGFR/ErbB-2 抑制剂。
Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors.
机构信息
Department of Oncology Medicinal Chemistry, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA.
出版信息
Bioorg Med Chem Lett. 2009 Feb 1;19(3):817-20. doi: 10.1016/j.bmcl.2008.12.011. Epub 2008 Dec 7.
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 IC(50) values less than 1 microM against human tumor cells in vitro.
已经鉴定出两种新型噻吩嘧啶核心的强效和选择性双重 EGFR/ErbB-2 激酶抑制剂新系列。将噻吩嘧啶核心作为 4-苯胺基喹唑啉核心的等排体进行了评估，并且包含噻吩[3,2-d]嘧啶核心的几种类似物显示出体外对人肿瘤细胞的抗增殖活性，IC50 值小于 1μM。
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