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Synthesis and Anti-cancer Activities of Apigenin Derivatives

[ Vol. 10 , Issue. 7 ]


Xing Zheng, Liuying Yu, Jing Yang, Xu Yao, Wenna Yan, Shaowei Bo, Ya Liu, Yun Wei, Zhiyi Wu and Guan Wang   Pages 747 - 752 ( 6 )


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 µ M, 2.25±0.42 µ M, it was better than 5-FU (12.92±0.61 µ M, 9.56±0.16 µ M), which shows a potential compound for colorectal adenocarcinoma and leucocythemia.


Anti-cancer activities, apigenin, baker-venkataraman reaction, flavonoids, MTT method, SAR.


Institute of Pharmacy & Pharmacology, University of South China, Hengyang, 421001, China.

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