Medicinal Chemistry

Dimitra Hadjipavlou-Litina
Aristotle University of Thessaloniki


Synthesis and Anti-cancer Activities of Apigenin Derivatives

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


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

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

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Article Details

Year: 2014
Page: [747 - 752]
Pages: 6
DOI: 10.2174/1573406410666140307152557
Price: $58