A series of dihydrotriazine derivatives bearing 5-aryloxypyrazole moieties were designed, and their anticancer activities against three human cancer cell lines (SGC-7901, HepG-2 and MCF-7) and one non-cancer cell line (LO2) were explored using the MTT assay in vitro. Most of the compounds exhibited potent antiproliferative activities against the three cancer cell lines, with compound 10e (IC₅₀ = 2.12 µM) exhibiting the most potent antiproliferative activity against HepG-2 cells. Interestingly, autophagy was observed in the 10e-treated HepG-2 cells. Compound 10e also increased reactive oxygen species (ROS) levels and resulted in marked HepG-2 cells apoptosis. Further studies revealed that compound 10e could enhance the expression of Cl-PARP, Cl-caspase-3, and Cl-caspase-9. In addition, 10e triggered the formation of autophagosomes by promoting LC3-II and Beclin-1 expression. These results might be useful for exploring and developing dihydrotriazine derivatives as novel anticancer agents.

设计了一系列带有 5-芳氧基吡唑部分的二氢三嗪衍生物，并利用体外MTT 测定。大多数化合物对三种癌细胞系表现出有效的抗增殖活性，其中化合物10e (IC ₅₀  = 2.12 µM) 对 HepG-2 细胞表现出最有效的抗增殖活性。有趣的是，在10e处理的HepG-2 细胞中观察到自噬。化合物10e还增加了活性氧 (ROS) 水平并导致显着的 HepG-2 细胞凋亡。进一步的研究表明，化合物10e可以增强Cl-PARP、Cl-caspase-3和Cl-caspase-9的表达。此外，10e通过促进 LC3-II 和 Beclin-1 的表达触发了自噬体的形成。这些结果可能有助于探索和开发二氢三嗪衍生物作为新型抗癌剂。