Chinese Journal of Organic Chemistry ›› 2020, Vol. 40 ›› Issue (2): 440-446.DOI: 10.6023/cjoc201907012 Previous Articles     Next Articles


栾天a,b,c, 全哲山b, 方应权a, 杨宏静a   

  1. a 重庆三峡医药高等专科学校药学院 重庆 404120;
    b 延边大学药学院 吉林延吉 133002;
    c 沈阳医学院药学院 沈阳 110034
  • 收稿日期:2019-07-05 修回日期:2019-07-23 发布日期:2019-10-12
  • 通讯作者: 杨宏静
  • 基金资助:

Design, Synthesis and Antiproliferative Activity of Chrysin Derivatives Bearing Triazole Moieties

Luan Tiana,b,c, Quan Zheshanb, Fang Yingquana, Yang Hongjinga   

  1. a Department of Pharmacy, Chongqing Three Gorges Medical College, Chongqing 404120;
    b College of Pharmacy, Yanbian University, Yanji, Jilin 133002;
    c College of Pharmacy, Shenyang Medical College, Shenyang 110034
  • Received:2019-07-05 Revised:2019-07-23 Published:2019-10-12
  • Supported by:
    Project supported by the National Natural Science Foundation of China (No. 21662036).

Two series of novel chrysin derivatives were synthesized, and their antiproliferative activity was evaluated against six human cancer cell lines (MGC-803, BEL-7402, HepG2, HeLa, A549, and SGC-7901) using methyl thiazolyl tetrazolium (MTT) assay. Preliminary bioassay results indicated that 7-((1-(3-fluorophenyl)-1H-1,2,3-triazol-4-yl)methoxy)-5-hydroxy-2-phenyl-4H-chromen-4-one (1c) and 7-((1-(2-chlorophenyl)-1H-1,2,3-triazol-4-yl)methoxy)-5-hydroxy-2-phenyl-4H-chro-men-4-one (1g) exhibited significantly improved antiproliferative activities against the MGC-803 cell line when compared with the parent compound chrysin and the positive control drug 5-fluorouracil. It demonstrates that compounds 1c and 1g are potential agents for cancer therapy.

Key words: chrysin, synthesis, triazole, derivatives, antiproliferation