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Chinese Journal of Organic Chemistry >

2020 , Vol. 40 >Issue 3: 794 - 800

DOI: https://doi.org/10.6023/cjoc201908012

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

  • Zhang Luye ,
  • Zhang Yang ,
  • Bao Chongnan ,
  • Yang Peng ,
  • Li Erdong ,
  • Meng Yaqi ,
  • Cui Fei ,
  • Zhou Rui ,
  • Huang Shiyu ,
  • Zheng Jiaxin ,
  • Shan Lihong ,
  • Liu Hongmin ,
  • Zhang Qiurong
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  • 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 date: 2019-08-08

  Revised date: 2019-10-11

  Online 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).

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Abstract

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

Cite this article

Zhang Luye , Zhang Yang , Bao Chongnan , Yang Peng , Li Erdong , Meng Yaqi , Cui Fei , Zhou Rui , Huang Shiyu , Zheng Jiaxin , Shan Lihong , Liu Hongmin , Zhang Qiurong . Synthesis and Antitumor Activity of Novel 1,3-Disubstituted Pyridazinone Derivatives[J]. Chinese Journal of Organic Chemistry, 2020 , 40(3) : 794 -800 . DOI: 10.6023/cjoc201908012

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