| 三唑类白杨素衍生物的设计、合成及其抗增殖活性研究 |
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| 引用本文： | 栾天,全哲山,方应权,杨宏静. 三唑类白杨素衍生物的设计、合成及其抗增殖活性研究[J]. 有机化学, 2020, 0(2): 440-446 |
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| 作者姓名： | 栾天 全哲山 方应权 杨宏静 |
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| 作者单位： | 重庆三峡医药高等专科学校药学院;延边大学药学院;沈阳医学院药学院 |
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| 基金项目： | 国家自然科学基金(No.21662036)资助项目. |
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| 摘 要： | 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1c与1g具有深入研究用以开发抗癌药物的潜能.
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| 关 键 词： | 白杨素 合成 三唑 衍生物 抗增殖 |
Design,Synthesis and Antiproliferative Activity of Chrysin Derivatives Bearing Triazole Moieties |
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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, 0(2): 440-446 |
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| Authors: | Luan Tian Quan Zheshan Fang Yingquan Yang Hongjing |
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| Affiliation: | (Department of Pharmacy,Chongqing Three Gorges Medical College,Chongqing 404120;College of Pharmacy,Yanbian University,Yanji,Jilin 133002;College of Pharmacy,Shenyang Medical College,Shenyang 110034) |
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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)-1 H-1,2,3-triazol-4-yl)methoxy)-5-hydroxy-2-phenyl-4 H-chromen-4-one(1 c) and 7-((1-(2-chlorophenyl)-1 H-1,2,3-triazol-4-yl)methoxy)-5-hydroxy-2-phenyl-4 H-chromen-4-one(1 g) 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 1 c and 1 g are potential agents for cancer therapy. |
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| Keywords: | chrysin synthesis triazole derivatives antiproliferation |
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