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Anti-Cancer Agents in Medicinal Chemistry

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ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

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Letter Article

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

Author(s): Islam Zaki *, Sarah A. Eid , Mohamed S. Elghareb, Al-Shimaa M. Abas, Gaber Mersal and Faten Z. Mohammed

Volume 22, Issue 9, 2022

Published on: 12 January, 2022

Page: [1634 - 1642] Pages: 9

DOI: 10.2174/1871520621666211103105255

Price: $65

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.

Keywords: Acrylic acid, quinoline, cell cycle analysis, annexin V, CDK-2, MCF-7.

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