Background: Among seventeen compounds derived from chalcones investigated as potential anticancer drugs towards LN229 glioblastoma cell line, only two were effective.
Materials and methods: Anticancer activity was investigated by evaluating the cell growth, cell cycle, mitotic index and the cell death.
Results: Two compounds, namely C2 and C12, inhibited cell proliferation associated with a blockade in the G(2)/M phase of the cell cycle and arrested the growth of tumour spheroid mimicking in vivo tumour. C2 blocked cells in the G(2) phase whereas C12 blocked cells in the M phase of the cell cycle. C12 and C2 killed 40% and 95% of the cells respectively using complex mechanisms. The two compounds increased the fluorescence of rhodamine-123 and N-acetylcysteine inhibited their activity, suggesting a role for reactive oxygen species in cell death mediated by these two compounds.
Conclusion: C2 and C12 are markedly cytostatic and cytolytic to glioblastoma cells and act through different pathways.