Chinese Journal of Organic Chemistry ›› 2021, Vol. 41 ›› Issue (8): 3214-3222.DOI: 10.6023/cjoc202102030 Previous Articles     Next Articles



马姣丽a, 郭鹏虎a, 李静b, 廖新成b, 程辉成a,*()   

  1. a 广东石油化工学院化学学院 广东茂名 525000
    b 郑州大学化学与分子工程学院 郑州 450052
  • 收稿日期:2021-02-18 修回日期:2021-03-30 发布日期:2021-05-14
  • 通讯作者: 程辉成
  • 基金资助:
    国家自然科学基金(22078072); 广东省基础与应用基础研究基金(2019A1515110346); 茂名市科技计划(2019401); 茂名市科技计划(2020581); 广东石油化工学院博士生启动基金(517152); 广东石油化工学院博士生启动基金(2019rc053); 广东石油化工学院青年创新人才培养基金(517136)

Synthesis and Antitumor Activity of Amide Derivatives Containing 1,3,4-Thiadiazole and Pyrazole Moieties

Jiaoli Maa, Penghu Guoa, Jing Lib, Xincheng Liaob, Huicheng Chenga()   

  1. a College of Chemistry, Guangdong University of Petrochemical Technology, Maoming, Guangdong 525000
    b College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou 450052
  • Received:2021-02-18 Revised:2021-03-30 Published:2021-05-14
  • Contact: Huicheng Cheng
  • Supported by:
    National Natural Science Foundation of China(22078072); Guangdong Basic and Applied Basic Research Foundation(2019A1515110346); Science and Technology Plan of Maoming(2019401); Science and Technology Plan of Maoming(2020581); Doctor Startup Project of Guangdong University of Petrochemical Technology(517152); Doctor Startup Project of Guangdong University of Petrochemical Technology(2019rc053); Young Creative Talents Training Project of Guangdong University of Petrochemical Technology(517136)

In this work, a series of newly-synthesized amide derivatives (A1~A26) carrying 1,3,4-thiadiazole and pyrazole moieties were successfully designed and synthesized. In addition, their structures were characterized by multiple techniques including 1H NMR, 13C NMR, IR, ESI-MS and HRMS. Furthermore, based on the antitumor results against human hepatocarcinoma cells (HepG2) and human gastric carcinoma cells (MGC803) via methyl thiazolyl tetrazolium (MTT) method, the in vitro cytotoxic activities of the compounds were evaluated, indicating that compounds A1 (IC50=0.0695 μmol/mL), A2 (IC50=0.0682 μmol/mL) and A3 (IC50=0.0753 μmol/mL) exhibited similar inhibitory effect against HepG2 cells. More importantly, compound A1 displayed superior inhibition performance against MGC803 cells (IC50=0.0420 μmol/mL) compared with that of 5-fluorouracil (IC50=0.0820 μmol/mL).

Key words: amide derivatives, organic synthesis, 1,3,4-thiadiazole, pyrazole, antitumor activity