Synthesis of Citrus polymethoxyflavonoids and their antiproliferative activities on Hela cells
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A series of polymethoxyflavonoids (3–16) were synthesized through dehydrogenation, O-methylation, glycoside hydrolysis, bromination, microwave-assisted aromatic nucleophilic substitution, dimethyldioxirane oxidation and regioselective demethylation, starting from abundant and inexpensive natural sources naringin and hesperidin. All the synthetic compounds were test for antiproliferative activities on human cervical carcinoma Hela cell line by the standard CCK-8 assay, the result showed that most of the target compounds exhibited moderate to potent antiproliferative activities on Hela cells comparable with the positive control cis-Platin. Among them, 5-hydroxypolymethoxy flavonoid 13 showed the strongest activity (IC50 0.791 μM).
KeywordsPolymethoxyflavonoids Synthesis Antiproliferative activity Hela cells
We thank the National “Twelfth Five-year” plan for Science & Technology Support (NO. 2012BAD31B02) and the Hunan Provincial Natural Science Foundation of China (NO. 14JJ2048) for financial support.
Compliance with ethical standards
Conflict of interest
The authors declare that they have no competing interest.
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