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

[ Vol. 17 , Issue. 2 ]

Author(s):

Sanal Dev, Della Grace Thomas Parambi, Bency Baby, Githa Elizabeth Mathew, Hendawy Omnia Magdy, Monu Joy, Shine Sudev and Bijo Mathew*   Pages 138 - 144 ( 7 )

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.

Affiliation:

Department of Pharmaceutical Chemistry, Al Shifa College of Pharmacy, Perintalmanna, Kerala-679325, Department of Pharmaceutical Chemistry, Jouf University, Sakaka, Al Jouf-2014, Department of Pharmacognosy, Al Shifa College of Pharmacy, Perintalmanna, Kerala 679325, Department of Pharmacology, Grace College of Pharmacy, Kerala, Department of Clinical Pharmacology, Jouf University, Sakaka, Al Jouf-2014, School of Pure and Applied Physics, MG University, Kerala-686560, Department of Pharmaceutical Analysis, Moulana College of Pharmacy, Perintalmanna, Kerala 679322, Division of Drug Design and Medicinal Chemistry Research Lab, Department of Pharmaceutical Chemistry, Ahalia School of Pharmacy, Palakkad-678557, Kerala

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