Call for Papers   a href="https://bentham.manuscriptpoint.com/journals/acamc" class="submit_manuscript">Call for Papers  

Article Details


<i>In Vitro</i> Antitumor Evaluation of Acrylic Acid Derivatives Bearing Quinolinone Moiety as Novel Anticancer Agents

[ Vol. 22 , Issue. 9 ]

Author(s):

Islam Zaki *, Sarah A. Eid , Mohamed S. Elghareb, Al-Shimaa M. Abas, Gaber Mersal and Faten Z. Mohammed   Pages 1634 - 1642 ( 9 )

Abstract:


<P>Background: Due to the emergence of resistance to available anticancer agents, the demand for new cytotoxic agents has grown. <P> 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. <P> 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. <P> 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. <P> 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.</P>

Keywords:

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

Affiliation:

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Port Said University, Port Said, Chemistry Department, Faculty of Science, Port-said University, Port Said, Chemistry Department, Faculty of Science, Port-said University, Port Said, Chemistry Department (Biochemistry branch), Faculty of Science, Zagazig University, Zagazig, Department of Chemistry, College of Science, Taif University University, Taif 26571, Chemistry Department (Biochemistry branch), Faculty of Science, Zagazig University, Zagazig

Graphical Abstract:



Read Full-Text article