An Environment-friendly Synthesis of Piperonal Chalcones and Their Cytotoxic and Antioxidant Evaluation

Author(s): Sanal Dev, Della Grace Thomas Parambi, Bency Baby, Githa Elizabeth Mathew, Hendawy Omnia Magdy, Monu Joy, Shine Sudev, Bijo Mathew*

Journal Name: Letters in Drug Design & Discovery

Volume 17 , Issue 2 , 2020

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Graphical Abstract:


Background: Grindstone technique has been widely used as an efficient, consistent, more environmentally benign, solvent-free protocol for the preparation of many compounds with higher atom economy.

Methods: A series of fourteen piperonal chalcone compounds were synthesized by this method and characterized by physical and spectral data (FT-IR, 1H NMR, Mass and elemental analysis). All chalcones were evaluated for their cytotoxic action against the cancer cell lines, MCF-7 and HepG2. One 2-pyridyl-substituted compound 14 with IC50 values 17.4±0.2 towards MCF-7 and 15.4±0.6µmol L-1 towards HepG2 cells.

Results: The results demonstrated that the cytotoxic activity of 2-pyridyl-substituted compound shown higher activity as compared with the standard cisplatin towards HepG2 cells.

Conclusion: Compound 14 showed good antioxidant activities in the DPPH test and H2O2 assay (IC50 = 17.23± 33/µg/mL and 20.17± 0.33µg/mL) when compared with the standard ascorbic acid (IC50=µg/mL 18.26 ± 0.22and 21.66± 1.06 µg/mL).

Keywords: Grindstone chemistry, chalcones, cytotoxicity, antioxidant, DPPH test, cirplatin.

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Article Details

Year: 2020
Published on: 13 February, 2020
Page: [138 - 144]
Pages: 7
DOI: 10.2174/1570180815666181016155934
Price: $65

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