摘要/Abstract
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.
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
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