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
收藏
页码：747 / 752
页数：6
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