有机化学 ›› 2020, Vol. 40 ›› Issue (2): 440-446.DOI: 10.6023/cjoc201907012 上一篇    下一篇

研究论文

三唑类白杨素衍生物的设计、合成及其抗增殖活性研究

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 出版日期:2020-02-25 发布日期:2019-10-12
  • 通讯作者: 杨宏静 E-mail:40278667@qq.com
  • 基金资助:
    国家自然科学基金(No.21662036)资助项目.

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 Online:2020-02-25 Published:2019-10-12
  • Supported by:
    Project supported by the National Natural Science Foundation of China (No. 21662036).

合成了2个系列的白杨素衍生物,采用噻唑蓝(MTT)法测试了所有化合物针对六种肿瘤细胞的体外抗增殖活性,包括MGC-803,BEL-7402,HepG2,HeLa,A549以及SGC-7901细胞.实验结果显示,7-[1-(3-氟苯基)-1H-1,2,3-三唑-4-甲氧基]-白杨素(1c)与7-[1-(2-氯苯基)-1H-1,2,3-三唑-4-甲氧基]-白杨素(1g)针对MGC-803细胞的活性与先导化合物白杨素及阳性对照药5-氟尿嘧啶相比显著提高.因此,化合物1c1g具有深入研究用以开发抗癌药物的潜能.

关键词: 白杨素, 合成, 三唑, 衍生物, 抗增殖

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