1,2,3-三唑-1,3,4-噻二唑三氮烯类化合物的合成及生物活性研究  

Synthesis and Biological Activities of 1,2,3-Triazole-1,3,4-Thiadiazole Triazene Compounds

作　　者：陈彦君[1] 张明千 魏光璞 龙跃[2] CHEN Yan-jun;ZHANG Ming-qian;Wei Guang-pu;LONG Yue(Department of Chemical and Environmental Engineering,Jiaozuo Universiy,Jiaozuo 454003,China;College of Chemistry and Molecular Engineering,Zhengzhou University,Zhengzhou 450001,China)

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

出　　处：《化学试剂》2020年第6期646-651,共6页Chemical Reagents

基　　金：国家自然科学基金资助项目(J1210060);河南省科技攻关计划项目(0624420031);河南省基础研究基金资助项目(022463001);国家级大学生创新创业训练计划项目(2016xjxm253)。

摘　　要：将三氮烯结构与1,3,4-噻二唑、1,2,3-三唑环结构拼接,合成16个新型目标化合物,并通过1HNMR、IR和LC-MS等确定其结构。通过以典型三氮烯药物达卡巴嗪(DTIC)作参照,对人胃癌细胞(MGC803)、人前列腺癌细胞(PC3)和人肝癌细胞(HepG2)做活性检测,结果显示部分化合物表现出较好的抑制活性,其中2-((1-(4-甲氧基苯基)-1,2,3-三唑-4-基)甲硫基)-5-(4-(3,3-二甲基三氮烯-1-基)苯基)-1,3,4-噻二唑对人前列腺癌细胞(PC3)的IC50值为39.6μmol/L,远低于对照药达卡巴嗪。16 Novel title compounds were synthesized by combination of the triazene with 1,2,3-triazole,1,3,4-thiadiazole.The structures of the title compounds were determined by 1HNMR,IR and LC-MS.By using the typical triazene drug dacarbazine(DTIC)as the reference,the activity detections of human gastric cancer cells(MGC803),human prostate cancer cells(PC3)and human liver cancer cells(HepG2)were carried out.The results showed that some compounds displayed good inhibitory activity,the IC50 value of 2-(((1-(4-methoxyphenyl)-1H-1,2,3-triazol-4-yl)methyl)thio)-5-(4-(3,3-dimethyltriaz-1-en-1-yl)phenyl)-1,3,4-thiadiazole was 39.6μmol/L against human prostate cancer cells(PC3),which was far lower than the control drug DTIC.

关 键 词：三氮烯 1 3 4-噻二唑 1 2 3-三唑 人胃癌细胞 人前列腺癌细胞 人肝癌细胞 

分 类 号：O622.6[理学—有机化学]