Study of biocompatibility, cytotoxic activity in vitro of a tetrazole-containing derivative of 2-amino-4,6-di(aziridin-1-yl)-1,3,5-triazine

The hydrolytic stability, hemocompatibility, antioxidant properties and in vitro cytotoxic activity of {5-[(4,6-di(aziridin-1-yl)-1,3,5-triazin-2-yl)amino]-2,2-dimethyl-1,3-dioxan-5-yl}methyl 2-(5-phenyl-2H-tetrazol-2-yl)acetate have been studied. 1H NMR spectroscopy showed that this tetrazole-containing derivative of 1,3,5-triazine is stable in neutral (pH 7) and alkaline (pH 10) media; hydrolysis of the dioxane cycle occurs in an acidic environment (pH 3). It has been established that {5-[(4,6-di(aziridin-1-yl)-1,3,5-triazin-2-yl)amino]-2,2-dimethyl-1,3-dioxan-5-yl}methyl-2-(5-phenyl-2H-tetrazol-2-yl)acetate is hemocompatible, exhibits antioxidant properties, but does not show antiradical activity over the entire range of concentrations. In turn, the study of cytotoxic activity in vitro showed that the tetrazole-containing derivative of 1,3,5-triazine has an effect on the cell lines of human alveolar basal epithe-lium adenocarcinoma A549 (IC50 41.3 mu mol l-1), human ovarian teratocarcinoma PA-1 (IC5010.6 mu mol l-1), hepatocarcinoma Huh7 (IC50 19.9 mu mol l-1), cervical cancer HeLa (IC50 3.7 mu mol l-1), and human em-bryonic kidney HEK293 (IC5015.8 mu mol l-1). It was suggested one of the possible mechanism of substance 2 cytotoxicity via HIF pathway inhibition.

Automated summary

This study investigated the stability, compatibility, antioxidant properties, and cytotoxicity of a tetrazole-containing derivative of 1,3,5-triazine. The derivative showed stability in neutral and alkaline conditions, but undergoes hydrolysis in acidic environments. It exhibited good hemocompatibility and antioxidant properties, but did not exhibit antiradical activity. Furthermore, it demonstrated cytotoxic effects on various cancer cell lines, potentially through HIF pathway inhibition.