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 1,4-dihydropyridines (1,4-dhps) (4a,4b and 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-dialkyloxylcarbonyl,4-dihydropyridine-4-yl) benzene compounds (4a and 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 anticancer agents. © 2016 by school of pharmacy.