Synthesis and Anti-cancer Activities of Apigenin Derivatives
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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