Cytotoxicity of a new condensed benzimidazoledione derivative against tumor and normal cell lines

Condensed benzimidazoledione derivatives with a nodal nitrogen atom can become the basis for the development of clinical therapeutic agents for the effective treatment of oncological diseases. This requires research that includes the synthesis and study of the antitumor activity of compounds of this group.

The aim. Search for new cytotoxic agents from a series of condensed benzimidazole diones with a nodal nitrogen atom.

Materials and methods. The cytotoxic profile of the synthesized compound was evaluated using an MTT test based on the reduction reaction of tetrazolium salt (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide) by mitochondrial dehydrogenases of living cells to formazane crystals insoluble in water. The IC50 values of the cytotoxic effect, which are concentrations of a compound leading to the death of 50 % of cells in a sample, were determined as indicators of effectiveness.

Result. The cytotoxicity of a new benzimidazole derivative, 7-bromo-8-chloro-3,4-dihydro-1H-[1,4]oxazino[4,3-a]benzimidazole-6,9-dione, was demonstrated against two tumor cell lines: lung adenocarcinoma (A549) and breast adenocarcinoma (MCF-7). In turn, for normal human embryonic kidney cells (Hek-293), this compound was approximately 2.5 times less toxic.

Conclusions. The results indicate that fused benzimidazole derivatives with a nodal nitrogen atom are a promising class of compounds for the development of new antitumor agents with selective toxicity.

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