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

doi:10.6023/cjoc201907012

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

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

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 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 Tian^a,b,c, Quan Zheshan^b, Fang Yingquan^a, Yang Hongjing^a

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).

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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

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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.

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三唑类白杨素衍生物的设计、合成及其抗增殖活性研究

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

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