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Medicinal Chemistry
ISSN (Print): 1573-4064
ISSN (Online): 1875-6638
VOLUME: 10
ISSUE: 7
DOI: 10.2174/1573406410666140307152557      Price:  $58









Synthesis and Anti-cancer Activities of Apigenin Derivatives

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Author(s): Xing Zheng, Liuying Yu, Jing Yang, Xu Yao, Wenna Yan, Shaowei Bo, Ya Liu, Yun Wei, Zhiyi Wu and Guan Wang
Pages 747-752 (6)
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.
Affiliation:
Institute of Pharmacy & Pharmacology, University of South China, Hengyang, 421001, China.