Synthesis, anticancer activity, and apoptosis mechanism of some chalcone derivatives

The research for finding new cancer agents with good efficacy and low toxicity is still in demand because this disease is still counted as main cause of death worldwide. Chalcone derivatives are known as prospective sources to find potent anticancer agent. Some amino chalcone and coumarin chalcone derivatives have been successfully synthesized from the reaction of 4'-amino acetophenone, acetyl coumarin, and derivatives of benzaldehyde by Claisen-Schmidt reaction. The molecular structure of the prepared compounds was determined by spectroscopic evidence including IR, ESIMS, ¹H- and ¹³C-NMR. Anti-proliferative activity of the prepared compounds is examined using MTT reagent. Apoptosis and cell cycle inhibition were determined by the flow cytometer. Double staining using orange acridine - etidium bromide was used to determine morphologically cancer cells underwent apoptosis. The IC₅₀ value of anti-proliferative examination ranging from 30.4 μg/mL to more than 100 μg/mL toward T47D cells and from 27.5 μg/mL to more than 100 μg/mL toward HeLa cells. Compound 2 (E)-1-(4-aminophenyl)-3-(4-fluoro-phenyl)prop-2-en-1-one exhibited the most active anticancer activity through induction apoptosis mechanism. It caused cell cycle arrest at G0/G1 and G2/M phase both for HeLa cells and T47D cells. Additionally, it also blocks S phase for T47D cells.