Synthesis and Anti-cancer Activities of Apigenin Derivatives

Title:Synthesis and Anti-cancer Activities of Apigenin Derivatives

Volume: 10 Issue: 7

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Zheng Xing, Yu Liuying, Yang Jing, Yao Xu, Yan Wenna, Bo Shaowei, Liu Ya, Wei Yun, Wu Zhiyi and Wang Guan, Synthesis and Anti-cancer Activities of Apigenin Derivatives, Medicinal Chemistry 2014; 10 (7) . https://dx.doi.org/10.2174/1573406410666140307152557