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.
出处
《化学研究与应用》
CAS
CSCD
北大核心
2017年第3期289-293,共5页
Chemical Research and Application
关键词
吲哚衍生物
酰腙
合成
抗肿瘤活性
indole derivative
hydrazone
synthesis
antitumor activity
