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.
[http://dx.doi.org/10.1080/00397911.2010.493260]
[http://dx.doi.org/10.1039/C4RA05244G]
[http://dx.doi.org/10.1039/C39870000279]
[http://dx.doi.org/10.1080/00397910802664244]
[http://dx.doi.org/10.1039/b106677n] [PMID: 12240095]
[http://dx.doi.org/10.1021/ed070p598]
[http://dx.doi.org/10.1002/aoc.1177]
[http://dx.doi.org/10.1016/j.molstruc.2011.02.029] [PMID: 21552381]
[http://dx.doi.org/10.1016/j.inoche.2011.10.032] [PMID: 23440300]
[http://dx.doi.org/10.1016/j.ejmech.2010.01.060] [PMID: 20153559]
[http://dx.doi.org/10.1016/j.ejmech.2012.02.023] [PMID: 22386368]
[http://dx.doi.org/10.2174/1871520615666150518093144] [PMID: 25980813]
[http://dx.doi.org/10.1016/j.bionut.2014.04.003]
[http://dx.doi.org/10.2174/1570178612666150903213416]
[http://dx.doi.org/10.1016/j.bioorg.2015.07.001] [PMID: 26189013]
[http://dx.doi.org/10.1002/cmdc.201600122] [PMID: 27159243]
[http://dx.doi.org/10.2174/1871524915666151002124443] [PMID: 26429556]
[http://dx.doi.org/10.4103/0250-474X.151588] [PMID: 25767315]
[http://dx.doi.org/10.1016/j.ejmech.2011.03.055] [PMID: 21514012]
[http://dx.doi.org/10.1016/j.molstruc.2017.05.100]
[http://dx.doi.org/10.1016/S0891-5849(98)00315-3] [PMID: 10381194]
![Wayfinder Image](/images/wayfinder.jpg)