Chin. J. Org. Chem. ›› 2015, Vol. 35 ›› Issue (9): 1985-1990.DOI: 10.6023/cjoc201503034 Previous Articles     Next Articles



张应鹏a, 谭伟a, 杨云裳a, 孙世琪b, 郭慧琛b   

  1. a 兰州理工大学石油化工学院 兰州 730050;
    b 中国农业科学院兰州兽医研究所 兰州 730050
  • 收稿日期:2015-03-31 修回日期:2015-05-06 发布日期:2015-05-26
  • 通讯作者: 张应鹏
  • 基金资助:

    甘肃省自然科学基金(No. 2014GS03265)资助项目.

Syntheses and in vitro Antitumor Activities of N-Acetyl Pyrazolines and Diphenyl Etheryl N-Acetyl Bis-pyrazolines

Zhang Yingpenga, Tan Weia, Yang Yunshanga, Sun Shiqib, Guo Huichenb   

  1. a School of Petrochemical Engineering, Lanzhou University of Technology, Lanzhou 730050;
    b Lanzhou Veterinary Research Institute, Chinese Academy of Agricultural Sciences, Lanzhou 730046
  • Received:2015-03-31 Revised:2015-05-06 Published:2015-05-26
  • Supported by:

    Project supported by the Natural Science Foundation of Gansu Province (No. 2014GS03265).

Seven N-acetyl pyrazolines 2a~2g and seven N-acetyl bis-pyrazolines 4a~4g with diphenyl etheryl moiety were synthesized and characterized by 1H NMR,13C NMR, elemental analysis and ESI-MS, and their in vitro antitumor activities on A549, H1299 and MCF-7 were evaluated by 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl-2H-tetrazolium) (MTS) assay. The results showed those compounds exhibited potent antiproliferative effects on cancer cells, among them compound 3,3'-(4,4'-diphenyl ether)-5,5'-bi[1-acetyl-5-(benzo[d][1,3]dioxo-5-yl)-2-pyrazoline] (4e) showed significantly inhibited the growth of all three kinds of cancer cells, the IC50 values of A549, H1299 and MCF-7 were 16.91, 10.09, 10.97 μmol/L, respectively.

Key words: N-acetyl pyrazoline, N-acetyl bis-pyrazoline, diphenyl ether, antitumor