1,3,4-噻二唑三氮烯酰胺衍生物的合成及抗肿瘤活性研究  

Synthesis and Antitumor Activities of 1,3,4-Thiadiazole Triazene Amide Derivatives

作　　者：陈彦君[1] 张明千 李子秋 罗德福 李龙辉 俞婷婷 龙跃[2] Chen Yanjun;Zhang Mingqian;Li Ziqiu;Luo Defu;Li Longhui;Yu Tingting;Long Yue(Department of Chemical and Environmental Engineering,Jiaozuo Universiy,Jiaozuo,Henan 454003;College of Chemistry and Molecular Engineering,Zhengzhou University,Zhengzhou 450001;School of Pharmaceutical Sciences,Zhengzhou University,Zhengzhou 450001)

机构地区：[1]焦作大学化学与环境工程学院,河南焦作454003 [2]郑州大学化学与分子工程学院,郑州450001 [3]郑州大学药学院,郑州450001

出　　处：《有机化学》2019年第11期3283-3288,共6页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.J1210060);河南省科技攻关计划(No.0624420031);河南省基础研究基金(No.022463001)资助项目~~

摘　　要：把三氮烯结构与1,3,4-噻二唑、酰胺相拼接,合成了14个未见报道的1,3,4-噻二唑三氮烯酰胺衍生物,并用核磁共振谱(NMR)、红外光谱(IR)和高分辨质谱(HRMS)等方法对化合物结构进行表征.通过以典型三氮烯药物达卡巴嗪作参照,对人食管癌细胞(EC109)、人胃癌细胞(MGC803)和人前列腺癌细胞(PC-3)做活性检测,结果显示化合物8a, 8h, 8i,8k, 8l对人前列腺癌细胞(PC-3)的抑制活性最好,其IC50值分别为33.02, 34.05, 7.71, 4.82, 23.84μmol·L^-1,远低于对照药达卡巴嗪(IC50值为146.43μmol·L^-1).By splicing the triazene structure with 1,3,4-thiadiazole and amide, fourteen unreported 1,3,4-thiadiazole triazene amide derivatives were synthesized. The structures of these compounds were characterized by nuclear magnetic resonance(NMR), infrared spectroscopy(IR) and high-resolution mass spectrometry(HRMS). By using the typical triazene drug dacarbazine as a reference, the activity detections of human esophageal cancer cells(EC109), human gastric cancer cells(MGC803) and human prostate cancer cells(PC-3) were carried out. The results showed that compounds 8a, 8h, 8i, 8k, and 8l had the best inhibitory activity against human prostate cancer cells(PC-3). And their IC50 values were 33.02, 34.05, 7.71, 4.82, 23.84 μmol·L^-1, which were far lower than the control drug their IC50 values were 33.02, 34.05, 7.71, 4.82, 23.84 μmol·L^-1, which were far lower than the control drug dacarbazine(146.43 μmol·L^-1).

关 键 词：三氮烯 1 3 4-噻二唑 酰胺 人食管癌细胞 人胃癌细胞 人前列腺癌细胞 

分 类 号：R73[医药卫生—肿瘤]