assessment of the cytotoxic effect of a series of 1,4-dihydropyridine derivatives against human cancer cells

cancer is a leading cause of death worldwide. despite the availability of several chemotherapeutic drugs, there is still a great need for more efficient agents for a better management of cancer. in this contribution, a series of 11 dhps (4a, 4b & 7a-i) were synthesized and evaluated for their cytotoxic effect against mcf-7, ls180, and molt-4 cancer cell lines using mtt assay. synthesized 2,6-dimethyl-3,5-bis-n-(aryl/heteroaryl) carbamoyl-4-aryl-1,4-dihydropyridines exhibited different potencies ranging from weak to good cytotoxic activities, while no activity could be recorded for 1,4-bis(2,6-dimethyl-3,5-dimethoxylcarbonyl-1,4-dihydropyridine-4-yl) benzene compounds (4a & 4b). tested dhp derivatives were more potent against molt-4 cells, when compared to ls180 and mcf-7 cells. compounds 7d (ic50=28.5±3.5 µm), 7a (ic50=29.7±4.7 µm) and 7a (ic50=17.4±2.0 µm) were the most potent derivatives against mcf-7, ls180 and molt-4 cells, respectively. it appeared that the introduction of n-thiazolyl carbamoyl group at the c3 and c5 positions of dhp ring enhanced the cytotoxic potential of these derivatives (compounds 7a-e). the findings of this study suggest that some of the thiazole substituted 1,4-dhps may be candidates for further modifications towards the discovery of potent antitumoral agents.