4,6-diaryl Pyrimidones as Constrained Chalcone Analogues: Design, Synthesis and Evaluation as Antiproliferative Agents
4,6-diarylpyrimidones as constrained chalcone analogues have been synthesised in the present study.
The synthesised compounds were evaluated against a panel of human cancer cell lines. Striking selectivity was
displayed by the compounds against MiaPaCa (Pancreatic) cell lines while PC-3 (prostate) and A-549 (lung) cell
lines were almost resistant to the exposure of the test compounds. Compound SK – 25 exhibited remarkable
cytotoxicity against MiaPaca-2 cell line with an IC50 value of 1.95 µM and was found to induce apoptosis
evidenced through phase contrast microscopy, DAPI staining and mitochondrial membrane potential loss. The cell
phase distribution studies indicated that the apoptotic population increased from 1.79% in control sample to 30.33
% in sample treated with 20 µM compound SK-25.
Keywords: Apoptosis, cell cycle, chalcone, contrained, cytotoxic, pyrimidones.
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