Synthesis and antiproliferative activity of novel aminoalkylated flavones

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 IC 50 values of 6.95–64.50 μΜ.