Synthesis and Anti-cancer Activities of Apigenin Derivatives

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


Volume 10, 8 Issues, 2014


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Medicinal Chemistry

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Editor-in-Chief:
Atta-ur-Rahman, FRS
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: mc@benthamscience.org

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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 and Guan Wang

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

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

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Article Details

Volume: 10
First Page: 1
Last Page: 6
Page Count: 6
DOI: 10.2174/1573406410666140307152557
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