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SYNTHESIS AND ANTIPROLIFERATIVE ACTIVITY OF NOVEL AMINOALKYLATED FLAVONES

Lili Yan, Haoran Liu, Qiuan Wang, Gangqiang Wang
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Abstract


Naturally occurring 5-hydroxy-4',7-dimethoxyflavone (acacetin-7-O-methyl ether) was synthesized through dehydrogenation, glycoside hydrolysis, and selective O-methylation, using naringin as starting material. Two series of sixteen novel aminoalkylated flavones were synthesized from 5-hydroxy-4',7-dimethoxyflavone. Furthermore, antiproliferative activity of the compounds was evaluated in vitro on a panel of three human cancer cell lines (HeLa, HCC1954, and SK-OV-3) using Cell Counting Kit-8 assay. The result showed that most of the synthetic compounds exhibited moderate to potent antiproliferative activities against the three human cancer cell lines with IC50 values of 6.95–64.50 μΜ.

Keywords


5-hydroxy-4',7-dimethoxyflavone; aminoalkylated flavones; antiproliferative activity; cancer cells; synthesis

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