含芳基酰胺考布他汀衍生物的合成及其抗肝癌细胞活性研究  

Synthesis and anti-hepatocarcinoma cell activity of combretastatin derivatives containing arylamide

作　　者：陈志豪 许润梅 秦巍 金耶智 李媛 田玉顺[1] CHEN Zhihao;XU Runmei;QIN Wei;JIN Yezhi;LI Yuan;TIAN Yushun(Yanbian University College of Pharmacy,Yanji 133002,Jilin,China)

机构地区：[1]延边大学药学院,吉林延吉133002

出　　处：《延边大学医学学报》2021年第2期96-100,共5页Journal of Medical Science Yanbian University

基　　金：国家自然科学基金项目(No.81260226);2021年国家级大学生创新创业训练计划项目(No.202110184063)。

摘　　要：[目的]获得安全并具有良好抗肝癌细胞活性的新型候选化合物.[方法]合成一系列含芳基酰胺考布他汀衍生物并验证其结构,采用MTT法检测所合成的化合物对人肝癌细胞株BEL-7402和HepG-2及人正常肝细胞L-02的抗增殖活性.[结果]所合成的一系列含芳基酰胺考布他汀衍生物中多数化合物对人肝癌细胞株BEL-7402表现出良好的抑制活性,其中(Z)-N-(4-(2-氰基-2-(3,4,5-三甲氧基苯基)乙烯基)苯基)-3,4,5-三甲氧基苯甲酰胺(8g)显示出最佳的抗肝癌细胞活性,且对人正常肝细胞的毒性较小.[结论]所合成的化合物8g具有良好的抗肝癌细胞活性.OBJECTIVE To obtain novel candidate compounds with safety and good anti-hepatocarcinoma cell activity. METHODS A series of novel combretastatin derivatives containing arylamides were synthesized and their structures were verified. MTT assay was used to detect the antiproliferative activity of the synthesized compounds against human hepatocarcinoma cell line BEL-7402 and HepG-2 and human normal hepatic cell L-02. RESULTS Most of the compounds in a series of synthesized combretastatin derivatives containing arylamides exhibited good inhibitory activities against BEL-7402, among them,(Z)-N-(4-(2-cyano-2-(3,4,5-trimethoxyphenyl) vinyl)phenyl)-3,4,5-trimethoxybenzamide(8 g) showed the best anti-hepatocarcinoma cell activity, and was less toxic to human normal hepatocytes. CONCLUSION The synthesized compound 8 g has good anti-hepatocarcinoma cell activity.

关 键 词：考布他汀衍生物 芳基酰胺 抗肝癌 选择性抑制活性 MTT法 

分 类 号：R914.5[医药卫生—药物化学] R965.1[医药卫生—药学]