吲哚乙酰腙类化合物的合成及体外抗肿瘤活性研究  

Synthesis and antitumor activity of indole-acetyl hydrazones

作　　者：李震[1] 邢秀梅 余湖长 李子成[1] 

机构地区：[1]四川大学化工学院,四川成都610065 [2]浙江新和成股份有限公司,浙江绍兴312500

出　　处：《化学研究与应用》2017年第3期289-293,共5页Chemical Research and Application

摘　　要：5-氨基-1-甲基-1H-吲哚与对氟苯磺酰氯反应,得到4-氟-N-(1-甲基-5-吲哚基)苯磺酰胺,再通过Vielsmeir反应得到4-氟-N-(3-甲酰基-1-甲基-5-吲哚基)苯磺酰胺,最后与苯并咪唑乙酰肼反应得到目标化合物5a^5g,并采用IR,~1H NMR和MS对其结构进行了确证。采用MTT法测试了目标化合物对A549、MDA、A375和HCT116四种癌细胞的体外抗肿瘤活性。Intermediate 4 was obtained by 5-amino-1-methyl-1H-indole reacted with4-fluorobenzenesulfonyl chloride,then formylated with DMF and POCl_3. The target compounds were synthesized by 4 and 2-（ 2-substitutedbenzimidazol-1-yl） acetyl hydrazides with acetic acid as catalyst.The structure of all compounds were characterized by ^1 H NMR,IR,and MS,and their antitumor activities against four cancer cells were determined by the MTT assay.

关 键 词：吲哚衍生物 酰腙 合成 抗肿瘤活性 

分 类 号：O626.2[理学—有机化学]