Synthesis and Anti-cancer Activities of Apigenin Derivatives

被引：13

作者：

Zheng, Xing ^{[1
,2
]}

Yu, Liuying ^{[1
]}

Yang, Jing ^{[2
]}

Yao, Xu ^{[1
]}

Yan, Wenna ^{[1
]}

Bo, Shaowei ^{[1
]}

Liu, Ya ^{[1
]}

Wei, Yun ^{[1
]}

Wu, Zhiyi ^{[3
]}

Wang, Guan ^{[3
]}

机构：

[1] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China

[2] Bur Commod Qual Supervis & Inspect, Hengyang 421001, Peoples R China

[3] Univ South China, Res Interest Grp, Hengyang 421001, Peoples R China

来源：

MEDICINAL CHEMISTRY | 2014年 / 10卷 / 07期

基金：

中国国家自然科学基金;

关键词：

Anti-cancer activities; apigenin; baker-venkataraman reaction; flavonoids; MTT method; SAR; HUMAN LEUKEMIA-CELLS; ANTITUMOR-ACTIVITY; COLORECTAL-CANCER; CYCLE ARREST; FLAVONOIDS; APOPTOSIS; TRIFLUOROMETHYLATION; PROLIFERATION; QUERCETIN; LUTEOLIN;

D O I：

10.2174/1573406410666140307152557

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of apigenin derivatives with phloroglucinol or resorcinol as raw materials were synthesized according to Baker-Venaktaraman reaction and their in vitro inhibitory activities on colorectal adenocarcinoma (HT-29) and leucocythemia (HL-60) cell lines were evaluated by the standard methyl thiazole tetrazolium (MTT) method. The results of biological test showed that some of apigenin derivatives possessed stronger anti-cancer activities than apigenin. Compound 6 showed the strongest activity against colorectal adenocarcinoma (HT-29) and leucocythemia (HL-60) cell lines with IC50 valure of 2.03 +/- 0.22 mu M, 2.25 +/- 0.42 mu M, it was better than 5-FU (12.92 +/- 0.61 mu M, 9.56 +/- 0.16 mu M), which shows a potential compound for colorectal adenocarcinoma and leucocythemia.

引用

页码：747 / 752

页数：6

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