Synthesis and Anti-cancer Activities of Apigenin Derivatives

ISSN: 1875-6638 (Online)
ISSN: 1573-4064 (Print)

Volume 11, 8 Issues, 2015

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Medicinal Chemistry

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Synthesis and Anti-cancer Activities of Apigenin Derivatives

Medicinal Chemistry, 10(7): 747-752.

Author(s): Xing Zheng, Liuying Yu, Jing Yang, Xu Yao, Wenna Yan, Shaowei Bo, Ya Liu, Yun Wei, Zhiyi Wu and Guan Wang.

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


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.

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Article Details

Volume: 10
Issue Number: 7
First Page: 747
Last Page: 752
Page Count: 6
DOI: 10.2174/1573406410666140307152557

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