三唑硫酮双席夫碱类衍生物的合成及其抗肿瘤活性研究  

Synthesis and antitumor activity evaluation of the derivatives of 1,2,4-triazole-5-thione bis-schiff base

作　　者：李敏[1] 张玉娜[1] 田玉顺[1] 

机构地区：[1]延边大学药学院药物化学教研部,吉林延吉133002

出　　处：《药学研究》2016年第7期376-378,389,共4页Journal of Pharmaceutical Research

基　　金：国家自然科学基金(No.81260226)

摘　　要：目的设计和合成一系列新的1,2,4-三唑-5-硫酮双席夫碱类衍生物并测定其抗肿瘤活性。方法以3,4,5-三甲氧基苯甲醛和甘氨酸为原料经一系列反应合成目标化合物7a^7g,经氢谱核磁共振(1H-NMR)和红外光谱(IR)表征后在He La、HCT116及BEL-7402细胞中用噻唑蓝(MTT)法测定其抑制细胞增殖的程度初步判断化合物的体外抗癌活性。结果相对于阳性对照药顺铂,化合物7a、7b、7d、7e和7g对HCT116细胞显示出显著的增殖抑制活性,7a和7d对He La细胞有明显的增殖抑制活性,而7d对BEL-7402细胞有很强的抑制作用。结论化合物7d对3种肿瘤细胞都有显著的抑制增殖活性,但其他化合物对不同来源肿瘤细胞显示出不同的抑制能力。Objective To design and synthesize a series of new derivatives of 1,2,4 - triazole - 5 - thione bis - schiff base and detect their antitumor activities in vitro. Methods the target molecules（7a ~ 7g）were synthesized by a series of reaction. The structures were characterized by 1 H - NMR and IR,and the growth inhibitory activities in vitro were evaluated by MTT assay against HeLa,HCT116 and BEL - 7402 cells. Results Compared with the positive control DDP,compound 7a,7b,7d,7e and 7g expressed significant stronger anti - proliferation effects against HCT116 cells,and 7a and 7d showed obvious inhibitory activities against HeLa cells,and BEL - 7402 cells,7d displayed the most significant inhibitory activity. Conclusion Compound 7d expressed significant anti - tumor activities in vitro against the three kinds cancer cells. Howev-er,the other compounds showed different inhibitory activities against tumor cell lines obtained from different tissues.

关 键 词：1 2 4 - 三唑 - 5 - 硫酮衍生物 席夫碱 抗癌活性 噻唑蓝法 顺铂 

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