Synthesis and anticancer activity of some 1-(2-aryl-2-oxoethyl)-2-[(morpholine-4-yl)thioxomethyl] benzimidazole derivatives

The synthesis of some new 1-(2-aryl-2-oxoethyl)-2-[(morpholine-4-yl)thioxomethyl]benzimidazole derivatives and investigation of their anticancer activities were aimed in this work. Thus, 2-[(morpholine-4-yl)thioxomethyl]benzimidazole was synthesized from 2-(chloromethyl)benzimidazole by Willgerodt-Kindler reaction, then it was reacted with some ? -bromoacetophenone derivatives in acetone in the presence of potassium carbonate to give final products. The structure of the compounds obtained were elucidated by using FT-IR, 1H-NMR, 13C-NMR and MS spectral data analysis results.Anticancer activity studies of the compounds were evaluated against C6, MCF-7 ve A549 tumor cell lines. The activity of the compounds were measured with MTT, BrdU method and using flow cytometry. According to the activity results, it was observed that the compounds showed greater activity on MCF-7 and C6 cells than A549 cells and the most active compounds were 6, 7, 9 and 12. It was also seen that the compound 9 bearing 4-chloro substituent on phenyl ring, had greater activity on C6 and A549 cell lines comparing with standard drugs Cisplatin and Doxorubicin.