Synthesis, Characterization, and Biological Evaluation of Novel Naringenin Derivatives as Anticancer Agents

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Author(s): Yogesh Murti*, Pradeep Mishra.

Journal Name: Current Bioactive Compounds

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Background: Cancer is a multifactorial heterogeneous disease and it is one of the major causes of mortality worldwide. Naringenin as one of the flavonoids has been reported to exhibit an anti-cancer activity. Based on the literature survey, a series of substituted naringenin derivatives was synthesized by using Claisen–Schmidt reaction with grinding technique.

Methods: Upon synthesis of compounds, the characterization of synthesized compounds was made using IR, NMR, Mass spectroscopy and elemental analysis. These derivatives were screened for anticancer activity on breast (MCF-7) and colon (HT-29) cell lines using sulforhodamine B (SRB) assay.

Results: Results displayed improved inhibitory concentration (IC50) values of naringenin derivatives. IC50 values of 3(4-chlorobenzylidene)-5,7-dihydroxy-2(4-hydroxyphenyl)chroman-4-one are 10.35 µM (MCF-7) & 12.03 µM (HT-29), which is most potent compound in the series. These finding confirms the suitability of 3-substituted naringenin in improving the anticancer effect.

Conclusion: Due to the intense interest in the development of drugs capable of inhibiting cancerous cells, naringenin derivatives may represent important precursor molecules for the therapeutic armamentarium of colon and breast cancer. Further structural modification in these structures will be of interest and may result in compounds having a better anticancer activity.

Keywords: Claisen–Schmidt reaction, Grinding Technique, Naringenin, Colon and Breast Cancers

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(E-pub Ahead of Print)
DOI: 10.2174/1573407215666181214114927
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