Abstract：
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 epithelium adenocarcinoma A549 (IC50 41.3 μmol l-1), human ovarian teratocarcinoma PA-1 (IC50 10.6 μmol l-1), hepatocarcinoma Huh7 (IC50 19.9 μmol l-1), cervical cancer HeLa (IC50 3.7 μmol l-1), and human embryonic kidney HEK293 (IC50 15.8 μmol l-1). It was suggested one of the possible mechanism of substance 2 cytotoxicity via HIF pathway inhibition.
摘要：
水解稳定性，血液相容性,研究了{5-[（4,6-二（氮丙啶-1-基）-1,3,5-三嗪-2-基）氨基]-2,2-二甲基-1,3-二恶烷-5-基}甲基2-（5-苯基-2H-四唑-2-基）乙酸酯的抗氧化特性和体外细胞毒性活性。1HNMR光谱表明，这种1,3,5-三嗪的含四唑衍生物在中性（pH7）和碱性（pH10）介质中稳定；二恶烷循环的水解发生在酸性环境（pH3）中。已经确定{5-[(4,6-二(氮丙啶-1-基)-1,3,5-三嗪-2-基)氨基]-2,2-二甲基-1,3-二恶烷-5-基}甲基-2-(5-苯基-2H-四唑-2-基)乙酸酯是血液相容性的，表现出抗氧化性能，但在整个浓度范围内没有抗自由基活性。反过来,体外细胞毒活性研究表明，含1,3,5-三嗪的四唑衍生物对人肺泡基底上皮腺癌A549细胞系有影响（IC5041.3μmoll-1），人卵巢畸胎癌PA-1（IC5010.6μmoll-1），肝癌Huh7（IC5019.9μmoll-1），宫颈癌HeLa（IC503.7μmoll-1），和人胚肾HEK293（IC5015.8μmoll-1）。提示物质2通过抑制HIF途径产生细胞毒性的可能机制之一。
