Jiang Guo-Wei, Chang Qing, Liang Dong-Yu, Zhang Yu-Ting, Meng Yong-Jun, Yi Qing-Qing
Pharmacy Department, Jiading District Central Hospital Affiliated Shanghai University of Medicine & Health Sciences, Shanghai, China.
Clinical Research Center, Jiading District Central Hospital Affiliated Shanghai University of Medicine & Health Sciences, Shanghai, China.
J Int Med Res. 2020 Feb;48(2):300060520903874. doi: 10.1177/0300060520903874.
The purpose of this paper was to synthesize 4-amino-1,2,4-triazole Schiff base derivative and to evaluate its antitumor activity.
2,4,6-Tris (4-formylphenoxy)-1,3,5-triazine was synthesized by nucleophilic substitution with reaction of -hydroxybenzaldehyde with cyanuric chloride. Then, the intermediate was reacted with 1,2,4-triazole to form 4-amino-1,2,4-triazole Schiff base derivative by reduction and ammonification of aldehydes. The 4-amino-1,2,4-triazole Schiff base derivative was characterized by infrared spectroscopy, nuclear magnetic resonance, and elemental analyses. Finally, the anticancer effect of 4-amino-1,2,4-triazole Schiff base derivative was evaluated by MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay on a lung adenocarcinoma cell line (A549) and a human hepatoma cell line (Bel7402).
The product synthesized in this study was confirmed to be 4-amino-1,2,4-triazole Schiff base derivative, and it significantly suppressed the proliferation of cancer cell lines in a dose-dependent manner.
We successfully prepared 4-amino-1,2,4-triazole Schiff base derivative and verified its antitumor activity.
本文旨在合成4-氨基-1,2,4-三唑席夫碱衍生物并评估其抗肿瘤活性。
通过对羟基苯甲醛与三聚氯氰的亲核取代反应合成2,4,6-三（4-甲酰基苯氧基）-1,3,5-三嗪。然后，使该中间体与1,2,4-三唑反应，通过醛的还原和氨化反应形成4-氨基-1,2,4-三唑席夫碱衍生物。通过红外光谱、核磁共振和元素分析对4-氨基-1,2,4-三唑席夫碱衍生物进行表征。最后，采用MTT [3-（4,5-二甲基噻唑-2-基）-2,5-二苯基四氮唑溴盐]法，在肺腺癌细胞系（A549）和人肝癌细胞系（Bel7402）上评估4-氨基-1,2,4-三唑席夫碱衍生物的抗癌效果。
本研究合成的产物被确认为4-氨基-1,2,4-三唑席夫碱衍生物，并且它以剂量依赖的方式显著抑制癌细胞系的增殖。
我们成功制备了4-氨基-1,2,4-三唑席夫碱衍生物并验证了其抗肿瘤活性。
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