Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (2): 451-456.DOI: 10.6023/cjoc201707025 Previous Articles     Next Articles



辛景超a,b, 栗娜a,b, 马启胜a,b, 李二冬a,b, 孟祥川a,b, 可钰a,b, 刘宏民a,b, 张秋荣a,b   

  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
  • 收稿日期:2017-07-22 修回日期:2017-09-29 发布日期:2017-10-20
  • 通讯作者: 可钰, 刘宏民, 张秋荣;;
  • 基金资助:


Synthesis and Antitumor Activity of 1-Phenyl-4-substituted Phthalazine Derivatives

Xin Jingchaoa,b, Li Naa,b, Ma Qishenga,b, Li Erdonga,b, Meng Xiangchuana,b, Ke Yua,b, Liu Hongmina,b, Zhang Qiuronga,b   

  1. a School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001;
    b Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou 450001
  • Received:2017-07-22 Revised:2017-09-29 Published:2017-10-20
  • Contact: 10.6023/cjoc201707025;;
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 81430085) and the Research Project of Science and Technology Bureau of Zhengzhou City (No. 141PQYJS554).

In order to find more efficient and economical antitumor drugs, a series of 1-phenyl-4-substituted phthalazine derivatives were synthesized and evaluated for antiproliferative activity in vivo. The structures of the synthesized compounds were confirmed by 1H NMR, 13C NMR and HRMS. The antitumor activity of the target compounds was performed against four cancer cell lines by 3-(4, 5-dimethyl-2-thiazolyl)-2, 5-diphenyl-2-H-tetrazolium bromide (MTT). The results showed that some compounds had a good antitumor activity, especially, N-(4-methoxyphenyl)-2-((4-phenylphthalazin-1-yl) thio) acetamide (5f) and N-(3-chloro-4-fluorophenyl)-2-(4-(4-phenylphthalazin-1-yl) piperazin-1-yl) acetamide (8c), exhibited better antitumor activities with IC50 values of 8.13 and 9.31 μmol•L-1 against the human esophageal cancer cells, which were superior to 5-fuorouracil.

Key words: synthesis, phthalazine derivative, antitumor activity