吲哚-2-碳酰肼衍生物的合成及抗肿瘤活性评价  

Synthesis and Antitumor Activity Evaluation of Indole-2-carbohydrazide Derivatives

作　　者：王宁伟 韩迎龙 张国强 黄学涛 刘明辉 杨烨鲜 王海君[1] 卜明 WANG Ning-wei;HAN Ying-long;ZHANG Guo-qiang;HUANG Xue-tao;LIU Ming-hui;YANG Ye-xian;WANG Hai-jun;BU Ming(School of Pharmacy,Qiqihar Medical University,Qiqihar 161006,China)

机构地区：[1]齐齐哈尔医学院药学院,黑龙江齐齐哈尔161006

出　　处：《化学试剂》2020年第8期926-930,共5页Chemical Reagents

基　　金：黑龙江省大学生创新创业训练计划项目(201911230035)。

摘　　要：以5-氯-吲哚-2-羧酸为原料,设计合成7个全新的吲哚-2-碳酰肼衍生物,并通过1HNMR、13CNMR和MS进行结构表征。采用四甲基偶氮唑盐(MTT)染色法对化合物的抗人结肠癌细胞(HCT116)、人乳腺癌细胞(MCF-7)和人肺癌细胞(A549)增殖活性进行评价。结果表明,5-氯-N′-((5-氟-1H-吲哚)-3-亚甲基)-1H-吲哚-2-碳酰肼对HCT116细胞具有显著抑制活性,IC50值为7.72μmol/L,同时发现该化合物能够呈浓度依赖方式诱导HCT116细胞凋亡。Using 5-chloroindole-2-carboxylic acid as starting material,seven indole-2-carbohydrazide derivatives had been synthesized,and their structures were confirmed by MS,1HNMR and 13CNMR.The antiproliferative activity of the compounds was evaluated against human colon cancer cells(HCT116),human breast cancer cells(MCF-7)and human lung cancer cells(A549)by methylthiazolyl tetrazolium(MTT)staining.The results showed that 5-chloro-N′-((5-fluoro-1H-indol-3-yl)methylene)-1H-indole-2-carbohydrazide displayed significant inhibitory activity against HCT116 cell lines with IC50 value of 7.72μmol/L.Furthermore,the compound could induce HCT116 cells apoptosis in a dose-dependent manner.

关 键 词：吲哚 碳酰肼 合成 抗肿瘤活性 凋亡 

分 类 号：O626[理学—有机化学]