Chinese Journal of Organic Chemistry ›› 2020, Vol. 40 ›› Issue (3): 731-739.DOI: 10.6023/cjoc201907052 Previous Articles     Next Articles


鄢龙家a, 黎永良a, 邓明高a, 陈安超a, 杜志云a, 董长治a,c, 陈惠雄a,b   

  1. a 广东工业大学轻工化工学院 广州 510006;
    b 巴黎笛卡尔大学生物医学系 巴黎 75006;
    c 巴黎狄德罗大学 巴黎 75013
  • 收稿日期:2019-07-30 修回日期:2019-09-21 发布日期:2020-04-02
  • 通讯作者: 陈惠雄
  • 基金资助:

Design, Synthesis and Biological Activities of Compounds Containing 1,3,4-Oxadiazole or 1,3,4-Thiadiazole

Yan Longjiaa, Li Yonglianga, Deng Minggaoa, Chen Anchaoa, Du Zhiyuna, Dong Changzhia,c, Chen Huixionga,b   

  1. a Faculty of Light Industry and Chemical Engineering, Guangdong University of Technology, Guangzhou, 510006, China;
    b Biomédicale, Université Paris Descartes, 75006 Paris, France;
    c Université Paris Diderot, 75013 Paris, France
  • Received:2019-07-30 Revised:2019-09-21 Published:2020-04-02
  • Supported by:
    Project supported by the National Natural Science Foundation of China (No. 21672043).

In order to find new anti-tumor drugs, a series of novel 1,3,4-oxadiazole and 1,3,4-thiadiazole derivatives were designed and synthesized. The target compounds were evaluated for antitumor activity in vitro on four human cancer cell lines including B-16 (skin melanoma cells), PC-3 (human prostate cancer cells), U87 (human primary glioblastoma cells) and A549 (human non-small cell lung cancer cells). The results displayed that some of the compounds had good activities, especially, 5-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-N-(2-methoxyphenyl)-1,3,4-thiadiazole-2-carboxamide (8b) and 5-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-N-(4-methoxyphenyl)-1,3,4-thiadiazole-2-carboxamide (8c) showed high antitumor activities against four cancer cell lines, which was better than dasatinib. These compounds were further studied for their possible target of tumor suppression.

Key words: 1,3,4-oxadiazole, 1,3,4-thiadiazole, anti-cancer, Src inhibitor