In Vitro Antitumor Evaluation of Acrylic Acid Derivatives Bearing Quinolinone Moiety as Novel Anticancer Agents.

BACKGROUND

Due to the emergence of resistance to available anticancer agents, the demand for new cytotoxic agents has grown.

OBJECTIVE

This study aims at synthesis and cytotoxic evaluation of new acrylic acid derivatives bearing quinolinone and halogenated quinolinone derivatives against three cancer cell lines.

METHODS

New acrylic acid derivatives bearing quinolinone and halogenated quinolinone moieties were synthesized and screened for their cytotoxic activity against breast MCF-7, liver HepG2, and colon HCT-116 cancer cell lines.

RESULTS

Molecules 3 and 8 showed the most potent cytotoxic activity against HCT-116. DNA flow cytometry assay showed cell cycle arrest at the G1 phase and cellular apoptosis. Moreover, molecules 3 and 8 showed cyclin-dependent kinase 2 (CDK2) inhibitory activity compared to the untreated control sample.

CONCLUSION

Acrylic acid derivatives bearing quinolinone and halogenated quinolinone moieties represent an important core and could be used as a lead for further development of drug compounds in order to achieve promising therapeutic results.