Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (6): 1516-1524.DOI: 10.6023/cjoc201712018 Previous Articles     Next Articles



宋永彬a,b, 李丹b, 杨异卉b, 纪红蕊a, 刘波a   

  1. a 哈尔滨理工大学化学与环境工程学院 哈尔滨 150040;
    b 哈尔滨医科大学药学院 哈尔滨 150081
  • 收稿日期:2017-12-10 修回日期:2018-01-22 发布日期:2018-02-06
  • 通讯作者: 杨异卉,
  • 基金资助:


Synthesis and Cytotoxicity of Dinaphtho [2, 1-b: 1', 2'-d]furan Derivatives

Song Yongbina,b, Li Danb, Yang Yihuib, Ji Hongruia, Liu Boa   

  1. a School of Chemical and Environmental Engineering, Harbin University of Science and Technology, Harbin 150040;
    b College of Pharmacy, Harbin Medical University, Harbin 150081
  • Received:2017-12-10 Revised:2018-01-22 Published:2018-02-06
  • Contact: 10.6023/cjoc201712018
  • Supported by:

    Project supported by the Youth Science Fund of Heilongjiang Province (No. QC2014C091), the University Nursing Program for Young Scholars with Creative Talents in Heilongjiang Province (No. 324015507) and the Heilongjiang Postdoctoral Scientific Research Developmental Fund (No. LBH-Q16187).

In order to study the structure-activity relationships of dinaphthofuran derivatives, two series of dinaphtho[2,1-b:1', 2'-d]furan derivatives were synthesized. The structures of all compounds were identified by 1H NMR, 13C NMR, HRMS and IR spectra. The in vitro antitumor activity of the synthesized derivatives was tested by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Most of them exhibited strong inhibitory activity on human hepatocellular carcinoma cell lines (HepG2 and SMMC-7721 cells), uterine cervix cancer Hela cells and acute promyelocytic leukemia NB4 cells. Compound 13k exhibited significant inhibitory activity against SMMC-7721 cells with IC50 vaue of 0.57 μmol·L-1, much lower than 20.21 μmol·L-1 of the positive control 5-Fu.

Key words: synthesis design, cytotoxicity, dinaphthofuran, NMR spectroscopy