In the present research, we developed pyrimidine-based hybridized molecules with either imidazole or triazole to find effective anticancer drugs. The reaction was accomplished using a multicomponent reaction pathway. The synthetics were explored for their utility as an anticancer agent via human topoisomerase-II and tubulin inhibition. Among the synthetics, compounds 1B4, 1B5, and 1B6 were potent anticancer agents tested in five cancer cell lines compared to colchicine and etoposide employed as positive controls. These synthetics were found further devoid of any significant cytotoxicity towards normal cells, thus proving their selective anticancer nature. Further, these compounds inhibited both the tubulin and hTopoII as indicated by in vitro-based assay. The mechanistic insights were corroborated using molecular docking studies. Besides this, the molecules were found to portray their secondary anticancer cell death mechanism via apoptosis. They decreased the oxidative stress, induced apoptosis, and arrested the cell cycle arrest at the G2/M phase in cancer cells.
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