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

Abstract

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.

• Authors: Islam Zaki, Sarah A Eid, Mohamed S Elghareb, Al-Shimaa M Abas, Gaber Mersal, Faten Z Mohammed
• Journal: Anti-cancer agents in medicinal chemistry (Anticancer Agents Med Chem) Vol. 22 Issue 9 Pg. 1634-1642 ( 2022) ISSN: 1875-5992 [Electronic] Netherlands
• PMID: 34732122 (Publication Type: Journal Article)
• Copyright: Copyright© Bentham Science Publishers; For any queries, please email at [email protected].

Chemical References

• Acrylates
• Antineoplastic Agents
• Quinolones
• acrylic acid

Topics

• Acrylates (pharmacology)
• Antineoplastic Agents
• Apoptosis
• Cell Line, Tumor
• Cell Proliferation
• Dose-Response Relationship, Drug
• Drug Screening Assays, Antitumor
• Humans
• Molecular Structure
• Quinolones (pharmacology)
• Structure-Activity Relationship