Synthesis and preliminary biological assessment of novel chalcone derivatives derived from Duff's formylated mephenesin

There is an urgent need in the medical community today for the discovery of anti-carcinogenic and anti-oxidative medicines that are more effective and have fewer adverse effects. To accomplish this goal, novel chalcone compounds (A1–A6) were produced by subjecting the Duff formylated mephenesin (I) and substituted aromatic ketones to a Claisen-Schmidt condensation reaction. Through the use of well-established spectroscopical techniques, the basic chemical structures of the produced derivatives were deduced. The MTT assay was used to determine how effective the produced chalcone derivatives were in vitro as neoplastic inhibitory agents against five different malignant cell lines, including HepG2, A549, MCF-7, HeLa, and Ovcar-3. In a similar manner, the anti-oxidative impact of chalcone derivatives was examined in vitro by making use of the DPPH moiety. According to the data, the derivative with the potent electronegative substituent, A2, exhibited the most potent anti-neoplastic impact compared to the other derivatives, with 50% inhibitory concentration (IC50) values that were quite near to those of the gold standard (doxorubicin). This effect was shown especially in relation to the HepG2 and A549 cells. In addition, the derivative A2 showed that it had a significant antioxidative impact on the examined free radical moieties, with percentage inhibition (Pi) values that were close to those of the standard (ascorbic acid).