Chinese Journal of Organic Chemistry ›› 2020, Vol. 40 ›› Issue (3): 794-800.DOI: 10.6023/cjoc201908012 Previous Articles     Next Articles


张路野a,b, 张洋a,b, 包崇男a,b, 杨鹏a,b, 李二冬a,b, 孟娅琪a,b, 崔飞a,b, 周蕊a,b, 黄诗雨a,b, 郑甲信a,b, 单丽红a,d, 刘宏民a,b,c,d, 张秋荣a,b,d   

  1. a 郑州大学药学院 郑州 450001;
    b 新药创制与药物安全性评价河南省协同创新中心 郑州 450001;
    c 省部共建食管癌防治国家重点实验室 郑州 450052;
    d 教育部药物制备关键技术重点实验室 郑州 450001
  • 收稿日期:2019-08-08 修回日期:2019-10-11 发布日期:2020-04-02
  • 通讯作者: 郑甲信, 单丽红, 刘宏民, 张秋荣;;;
  • 基金资助:

Synthesis and Antitumor Activity of Novel 1,3-Disubstituted Pyridazinone Derivatives

Zhang Luyea,b, Zhang Yanga,b, Bao Chongnana,b, Yang Penga,b, Li Erdonga,b, Meng Yaqia,b, Cui Feia,b, Zhou Ruia,b, Huang Shiyua,b, Zheng Jiaxina,b, Shan Lihonga,d, Liu Hongmina,b,c,d, Zhang Qiuronga,b,d   

  1. a School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001;
    b Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou 450001;
    c State Key Laboratory of Esophageal Cancer Prevention & Treatment, Zhengzhou University y, Zhengzhou 450052;
    d Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education of China, Zhengzhou 450001
  • Received:2019-08-08 Revised:2019-10-11 Published:2020-04-02
  • Supported by:
    Project supported by the National Natural Science Foundation of China (No. 81430085), the Natural Science Foundation of Henan Province (No. 182300410321), and the Openning Fund from State Key Laboratory of Esophageal Cancer Prevention & Treatment (No. K2020000X).

In order to find more efficient and low toxicity antitumor drugs, a series of novel 1,3-disubstituted pyridazinone derivatives were synthesized and evaluated for their antiproliferative activities against four human cancer cell lines (MCF-7, PC-3, SW-620 and HGC-27) in vitro. The results showed that most compounds had good antiproliferative activities, especially 2-(4-(4-bromophenyl)-1-oxo-tolylazine-2(1H)-yl)-N-(2-fluorophenyl)acetamide (5g) exhibited better antiproliferative activities with IC50 value of 6.01 μmol/L. In a nutshell, this work provided clues to discover antitumor agent based on the quinazoline scaffold.

Key words: pyridazinederiv, ative, synthesis, antiproliferative activity