Functionalized N-Pyridinylmethyl Engrafted Bisarylmethylidenepyridinones as Anticancer Agents

Abstract

Structurally interesting N-pyridinylmethyl engrafted bisarylmethylidenepyridinones with high functionality have been constructed in good yield. The structural interpretation of these compounds has been done with the aid of spectroscopic analysis and further established by single crystal X-ray diffraction studies. Following physical characterization, the synthesized compounds were tested for their in vitro anticancer activity against HepG2 cancer cells and it was found that all of the compounds exhibited some level of activity. We observed a significant level of cell viability losses to the cancer cells, while only smaller losses to the non-cancer cells were observed. Besides, the mechanistic investigation of toxicology revealed that the cancer cells were undergoing apoptotic pathway, induced by the generation of oxidative stress and the involvement of caspases. The analysis provides preliminary evidence for the successful control of cancer cells with a minimal effect on healthy normal cells because of the high IC50 levels and cell death mechanisms.