Novel 1,3,5‐triazine derivatives exert potent anti‐cervical cancer effects by modulating Bax, Bcl2 and Caspases expression

2018 
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.
    • Correction
    • Source
    • Cite
    • Save
    • Machine Reading By IdeaReader
    38
    References
    5
    Citations
    NaN
    KQI
    []