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Chinese Journal of Organic Chemistry >

2020 , Vol. 40 >Issue 2: 440 - 446

DOI: https://doi.org/10.6023/cjoc201907012

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

  • Luan Tian ,
  • Quan Zheshan ,
  • Fang Yingquan ,
  • Yang Hongjing
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  • 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 date: 2019-07-05

  Revised date: 2019-07-23

  Online published: 2019-10-12

Supported by

Project supported by the National Natural Science Foundation of China (No. 21662036).

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Abstract

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

Cite this article

Luan Tian , Quan Zheshan , Fang Yingquan , Yang Hongjing . Design, Synthesis and Antiproliferative Activity of Chrysin Derivatives Bearing Triazole Moieties[J]. Chinese Journal of Organic Chemistry, 2020 , 40(2) : 440 -446 . DOI: 10.6023/cjoc201907012

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