作为强效表皮生长因子受体（EGFR）抑制剂的取代6-炔基-4-苯胺基喹唑啉衍生物的合成与生物学评价
Synthesis and biological evaluation of substituted 6-alkynyl-4-anilinoquinazoline derivatives as potent EGFR inhibitors.
作者信息
Liu Lee Tai, Yuan Ta-Tung, Liu Hung-Huang, Chen Shyh-Fong, Wu Ying-Ta
机构信息
Development Center for Biotechnology, 102 Lane 169 Kang Ning Street, Xi Zhi, Taipei, Taiwan, ROC.
出版信息
Bioorg Med Chem Lett. 2007 Nov 15;17(22):6373-7. doi: 10.1016/j.bmcl.2007.08.061. Epub 2007 Aug 28.
A series of C-6 or C-3' alkynyl-substituted 4-anilinoquinazoline derivatives was prepared straightforwardly by a Sonogashira reaction of the corresponding bromo-substituted 4-anilinoquinazolines. Bioactive assay of these compounds for in vitro EGFR kinase inhibition demonstrated that the novel 6-hydroxypropynyl-4-anilinoquinazoline 5e was a very potent EGFR kinase inhibitor with an IC(50) of 14 nM.
通过相应的溴代4-苯胺基喹唑啉的Sonogashira反应直接制备了一系列C-6或C-3'炔基取代的4-苯胺基喹唑啉衍生物。这些化合物的体外表皮生长因子受体（EGFR）激酶抑制生物活性测定表明，新型6-羟基丙炔基-4-苯胺基喹唑啉5e是一种非常有效的EGFR激酶抑制剂，半数抑制浓度（IC50）为14 nM。
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