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The Thai Journal of Pharmaceutical Sciences

Abstract

Cancer remains a major class of morbidity and mortality despite basic and clinical research and trials of promising new therapies. In the current era, many drugs are marketed with flavonoid nucleus. Based on this information, this study aims to synthesize and screen flavones for their anticancer activity. Docking studies for cytotoxic activity of flavonoid derivatives targeting tankyrase enzyme were performed. A new series of flavonoid derivatives were prepared from chalcones. Chalcones were prepared between substituted benzaldehyde and 2-hydroxy acetophenone in the presence of potassium hydroxide as catalyst. The flavone derivatives were characterized based on IR, 1H NMR, and Mass spectral data. All the new compounds were subjected to antioxidant activity by 1,1-diphenyl-2-picrylhydrazyl and nitric oxide free radical scavenging activity. Cytotoxic activity was evaluated by MTT assay on two different cell lines. The antioxidant result reveals the potent antioxidant activity of compounds f4 and f6. Compounds mf6 and mf11 possess moderate activity. Cytotoxic activity results revealed that compound f10 have moderate activity and compound f4 shows potent cytotoxic activity on both MCF-7 and Hep-G2 cell line. The in vitro results suggest that some of the compounds showed potent antioxidant and cytotoxic activity. Compound f4 may be a promising cytotoxic molecule.

Publisher

Faculty of Pharmaceutical Sciences, Chulalongkorn University

First Page

646

Last Page

652

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