SYNTHESIS OF NEW TRIAZOLE AND THIADIAZOLE DERIVATIVES OF THE N,N'-DISUBSTITUTED BENZIMIDAZOLE-2-THIONE AND EVALUATION OF THEIR ANTITUMOR POTENTIAL.

In the present study series of triazole-, thiadiazole- and thiosemicarbazone-benzimidazole hybrid compounds were synthesized as potential anti-cancer agents. In order to determine their antitumor potential and cytotoxic effect (via MTT assay) lung adenocarcinoma (A549) and breast cancer (MDA-MB-231) cell lines were examined. For detection of apoptosis induced by drug treatment, DAPI staining was performed in order to observe the apoptotic alterations in cell nuclei. It was found that the thiadiazole derivative 12 leads to the occurrence of micronuclei, suggesting genotoxic effect. Furthermore, a wound healing assay was performed in order to test whether any changes in cell motility occurred upon treatment with the newly synthesized hybrids, since both cell lines are examples of highly invasive tumours. The cell motility of MDA-MB-231 was impeded mostly by compound 12 (15 % of wound closure) and in A549 compound 9 reduced cell motility by 46 % compared to the control. The obtained results suggest that compound 12 possesses a promising anticancer effect. [ABSTRACT FROM AUTHOR]