Study on the Synthesis and Antitumor Activity of Indolecarbazole Compounds Modified by Amino Acid and Piperidine  

作　　者：赵玲玲 祁刚 

机构地区：[1]College of Pharmacy, Nanjing University of Chinese Medicine [2]Jiangsu Key Laboratory of Biochemistry and Biotechnology of Marine Wetland, Yancheng Institute of Technology

出　　处：《Chinese Journal of Structural Chemistry》2017年第6期918-924,共7页结构化学（英文）

基　　金：Supported by the opening project of Jiangsu Key Laboratory of Biochemistry and Biotechnology of Marine Wetland(No.K2016-11)

摘　　要：A series of antitumor compounds with indolecarbazole structure modified by amino acid and piperidine were designed and synthesized. The indolecarbazole parent nucleus was firstly synthesized, condensed with bromine substituted amino acid methyl ester, then hydrolyzed and condensed with piperidine to produce the target compounds. In vitro cytotoxin activity test was performed against 7 target compounds with methylthiazolyldiphenyl-tetrazolium bromide（MTT）, and the results showed that compounds CZ-2, CZ-3 and CZ-5 have higher activity against human colon cancers（HT-29） and（HCT-8）, hepatocellular carcinoma（Bel-7402）, NSCLC（A549） and breast cancer（MCF-7） cells as compared with the positive control JDC-108.A series of antitumor compounds with indolecarbazole structure modified by amino acid and piperidine were designed and synthesized. The indolecarbazole parent nucleus was firstly synthesized, condensed with bromine substituted amino acid methyl ester, then hydrolyzed and condensed with piperidine to produce the target compounds. In vitro cytotoxin activity test was performed against 7 target compounds with methylthiazolyldiphenyl-tetrazolium bromide（MTT）, and the results showed that compounds CZ-2, CZ-3 and CZ-5 have higher activity against human colon cancers（HT-29） and（HCT-8）, hepatocellular carcinoma（Bel-7402）, NSCLC（A549） and breast cancer（MCF-7） cells as compared with the positive control JDC-108.

关 键 词：indolecarbazole  antitumor activity  cytotoxin activity 

分 类 号：O626[理学—有机化学]