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.
Keywords: Anti-cancer activities, apigenin, baker-venkataraman reaction, flavonoids, MTT method, SAR.
Medicinal Chemistry
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.
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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
DOI https://dx.doi.org/10.2174/1573406410666140307152557 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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