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

Abstract

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.

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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.

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