3-氰基-7-喹啉酰胺衍生物的合成和生物活性研究

Synthesis and biological evaluation of 3-quinolinecarbonitrile-7-amide derivatives

摘要:
以对甲基苯胺为原料, 设计合成了14个N-(6-甲基-3-氰基-4-芳胺基-7-喹啉) 酰胺衍生物, 其结构经EI-MS、¹H NMR、IR和元素分析确证。采用MTT法测试所合成化合物的体外抗肿瘤活性, 结果表明, 所合成的化合物均有一定的抗肿瘤作用, 其中化合物13j对胃癌细胞AGS的体外抑制活性优于EKB-569和Bosutinib, 抗肝癌细胞HepG2和结肠癌细胞HT-29的活性与阳性药相当。

Abstract:
A series of N-(3-cyano-6-methyl-4-anilinoquinoline-7-yl) amide derivatives 13a−13n have been synthesized, their structures were confirmed with ¹H NMR, EI-MS, IR and elemental analysis. Antitumor activities of all the synthesized compounds in vitro were tested with MTT. Compound 13j showed better than or equal antitumor activity on Bosutinib and EKB-569.