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A series of fluorinated chalcones ( 3a-f ) was synthesized and confirmed by several spectral tools. The cytotoxic effect of this series was tested against a panel of different cancer cell lines (MCF7, A549, HCT116, and PC3). MTT assay revealed that chalcone  3f  has the potent cytotoxic activity against all tested cancer cell lines except A549 cells. Chalcone  3f  showed the least cytotoxic activity against the normal epithelial cell line RPE-1 and the lowest IC 50  at 10.96 µM relative to the IC 50  of doxorubicin at 12.8 µM against the human breast cancer cell line MCF7. Molecular docking studies showed a good interaction of chalcone  3f  with the active site of histone demethylase (PLU-1/JARID1B) and Carboxy-terminal binding protein1 (CtBP1) proteins. Mechanistically, chalcone  3f  induced cell cycle arrest at G2/M phase and apoptosis assessed by flow cytometry, as well as DNA fragmentation in MCF7 cells. Chalcone  3f  upregulated mRNA expression levels of the apoptotic genes  BAX ,  p53 , and  Caspase-7, Caspase-8,  and  Caspase-9 , whereas mRNA expression levels of the antiapoptotic gene Bcl2, metastasis-related gene matrix metalloproteinase 1 ( MMP1 ), and the autophagic markers  ATG5  and  LC3B  were downregulated as quantified by qPCR. This study shows a cytotoxic effect of chalcone  3f  against cancer cells and emerges as a promising therapeutic drug against breast cancer.

polycyclic aromatic compounds

Cytotoxic Activity, Apoptosis Induction and Cell Cycle Arrest in Human Breast Cancer (MCF7) Cells by a Novel Fluorinated Tetrahydro-[1,2,4]Triazolo[3,4- a ]Isoquinolin Chalcones