3 years ago

Novel 1,3,5-Triazine Derivatives Exert Potent Anti-cervical Cancer Effects by Modulating Bax, Bcl2, and Caspases Expression

Novel 1,3,5-Triazine Derivatives Exert Potent Anti-cervical Cancer Effects by Modulating Bax, Bcl2, and Caspases Expression
Juan Zhang, Wanrong Wu, Xiwen Wang, Qiongying Lv, Wei Zhang, Yuexiong Yi, Kejia Wu
The present study aimed to develop novel 1,3,5-triazine derivatives as potent anti-cervical cancer agents. The compounds were synthesised in short steps with an excellent yield and characterised via various spectroscopic and analytical methods. A structure–activity relationship study suggested that electron-withdrawing substituents showed greater anticancer activity than electron-donating groups. Compound 7p (p-fluoro) showed the highest activity against cervical cancer cells. In a nude mouse xenograft model inoculated with HeLa cells, 7p showed dose-dependent inhibition of cervical tumour growth. Histopathological examination of excised tumour-bearing tissues showed that 7p improved the microstructure in a dose-dependent manner. Compound 7p also increased the proportions of HeLa cells in G0/G1 and S-phase and significantly decreased that of G2/M-phase. The effects of 7p on C-caspase-3, C-caspase-9, Bcl-2, and Bax expression in HeLa cells were also determined. This article is protected by copyright. All rights reserved. Structure–activity relationship study suggested that the halogen-containing compounds (F and Cl) had higher anticancer activity than non-halogen (OH, OCH3, and CH3) compounds.

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1111/cbdd.13133

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