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.
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We thank the National Natural Science Foundation of China (NO.J1210040) and Education Department of Hubei Province Science and Technology Research Project of China (NO.Q20162803) for the financial support.
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Supplementary information file containing analytical data characterizing the synthesized compounds and doseresponse curves is available at the journal website http://link.springer.com/journal/10593.
Published in Khimiya Geterotsiklicheskikh Soedinenii, 2017, 53(8), 871–875
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Yan, L., Liu, H., Wang, Q. et al. Synthesis and antiproliferative activity of novel aminoalkylated flavones. Chem Heterocycl Comp 53, 871–875 (2017). https://doi.org/10.1007/s10593-017-2132-7
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DOI: https://doi.org/10.1007/s10593-017-2132-7