Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (8): 2067-2075.DOI: 10.6023/cjoc201801001 Previous Articles     Next Articles



孙海燕a, 孙宏顺a, 刘明珍b, 黄伟b, 杨光富b   

  1. a 南京科技职业学院 南京 210048;
    b 华中师范大学化学学院 农药与化学生物学教育部重点实验室 武汉 430079
  • 收稿日期:2018-01-02 修回日期:2018-03-15 发布日期:2018-04-13
  • 通讯作者: 黄伟, 杨光富;
  • 基金资助:


Lead Optimization and Antiproliferative Activity Using a New Dithiocarbamates Substructure

Sun Haiyana, Sun Hongshuna, Liu Mingzhenb, Huang Weib, Yang Guangfub   

  1. a Nanjing Polytechnic Institute, Nanjing 210048;
    b Key Laboratory of Pesticide and Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079
  • Received:2018-01-02 Revised:2018-03-15 Published:2018-04-13
  • Contact: 10.6023/cjoc201801001;
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 201502063) and the Natural Science Foundation of Hubei Province (No. 2016CFB562).

In this work, a series of dithiocarbamate derivatives bearing diverse quinazolinones, benzoxazinones, and coumarin moieties were designed and synthesized via a one-pot three-component reaction. These compounds produced good yields and functioned quickly under mild conditions, and the desired products were readily isolated. Their in vitro antitumor activities were evaluated by the methyl thiazolyl tetrazolium (MTT) method against hepatoma carcinoma cells HCCLM-7, cervical carcinoma cells Hela, mammary adenocarcinoma cells MDA-MB-435S, colon carcinoma cells SW-480, laryngocarcinoma cells Hep-2, and mammary adenocarcinoma cells MCF-7. 3 compounds were identified as the most promising candidates, due to their high potency and broad-spectrum antiproliferative activity (IC50:3.5~13.5 μmol·L-1). The activities of some lead compounds were more than 10-fold more potent than that of positive control 5-fluorouracil (5-FU) (IC50:8.1~128.7 μmol·L-1). These results indicated that the dithiocarbamate (DTC) derivatives bearing fused heterocyclic moieties could be used as lead for further developing new antitumor active compounds.

Key words: dithiocarbamate, quinazolinone, benzoxazinone, coumarin, antiproliferative activity