4.7 Article

Dihydrotriazine derivatives display high anticancer activity and inducing apoptosis, ROS, and autophagy

Journal

BIOORGANIC CHEMISTRY
Volume 124, Issue -, Pages -

Publisher

ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2022.105813

Keywords

Dihydrotriazine derivatives; ROS levels; Autophagosomes; Anticancer agents

Funding

  1. Natural Science Foundation of Jilin Province [20210502028ZP]
  2. Department of Education of Jilin Province [JJKH20210495KJ]
  3. Zhoushan Science and Technology Bureau [2021C31044]

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A series of dihydrotriazine derivatives bearing 5-aryloxypyrazole moieties were designed and their anticancer activities were explored. Compound 10e exhibited the most potent antiproliferative activity against HepG-2 cells and induced autophagy and apoptosis. Further studies revealed enhanced expression of key proteins and autophagosome formation.
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 10(e) (IC50 = 2.12 mu M) 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.

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