Studies on the Synthesis and Anticancer Activity Investigation of Some 2-substitued-N-[4-(1-Methyl-4,5-Diphenyl-1H-Imidazole-2-yl)Phenyl] Acetamide Derivatives

Cancer is a progressive disease which can occur in different organs and systemsof body having no certain ethiopathology. Besides the methods such as surgeryand radiotherapy, another effective way that preferred for the treatment of canceris the use of chemotherapeutic agents. Thus, the studies are still being carried onto develop new chemotherapeutic agents which are probable to indicate activityon various cancer types.Imidazole is an important hetereocyclic ring participating in chemical structure ofnumerous drugs. It?s known that some drugs being used in cancer chemotherapycarries this ring system. There are lots of studies in literature aimed to synthesisand investigation of anticancer activities of mainly imidazole containingcompounds.In medicinal chemistry field, piperazine, benzazole (benzoxazole, benzothiazole)and azole (tetrazole, triazole, thiadiazole and thiazoline) ring systems are some ofthe other moieties that often subjected to studies to develop new chemotherapeuticagents.From this point, imidazole ring system was determined as the main structure andit was derived to carry azole, benzazole and piperazine ring systems via variouschemical reactions, in this study. Thus, seventeen novel compounds weresynthesized, containing two different pharmacophore groups on the samemolecule which are estimated to be responsible of the anticancer activity. Thestructures of obtained compounds were confirmed by the spectroscopic data ofinfrared (IR), nuclear magnetic resonance (NMR) and mass spectroscopy.To establish the relationship between anticancer activity and chemical structure,some physicochemical parameters of the compounds were evaluated and thecalculated values were used in quantitative structure activity relationships(QSAR) analysis.Anticancer activity tests were performed on colon (HT-29) and breast (MCF-7)carcinoma cell types. Test compounds, showed greater activity on HT-29 cellsthan MCF-7 cells. Compounds B6 and B7 were determined as the most effectivecompounds in the series. In order to obtain knowledge about genotoxicity of thesecompounds, mutagenity test was performed and it was determined that thecompounds were nonmutagen.