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Current Organic Synthesis

Editor-in-Chief

ISSN (Print): 1570-1794
ISSN (Online): 1875-6271

Research Article

Synthesis, Characterization and Preliminary Screening of New N-Substi-tuted -8-Methyl-4-Hydroxy-2-Quinolone -3-Carboxamides as Potential An-ticancer Agents

In Press, (this is not the final "Version of Record"). Available online 17 April, 2024
Author(s): Dania Altaher, Hiba Zalloum, Kamal Sweidan*, Dima A. Sabbah, Husam AlSalamat, Mahmoud Sunjuk and Reem Isleem
Published on: 17 April, 2024

DOI: 10.2174/0115701794291133240327044308

Price: $95

Abstract

Introduction: A new series of 4-hydroxy-8-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide derivatives has been synthesized in good yields, followed by complete characteri-zation using 1D-NMR, 2D-NMR, and IR techniques.

Methods: The final products contain amide, hydroxyl, and aromatic functional groups that usu-ally show significant bioactivity. The target products have been examined towards three cancer cell lines, namely colorectal cancer cell line (HCT116), breast cancer cell line (MCF-7), and leukemia cell line (K562) in addition to the fibroblast cells, that were used as a model for normal human tissue.

Results: The anticancer results signified that compound 6 showed the most activity in the series accomplished with IC50 values of 14.6, 5.3 and 12.8 μM,

Conclusion: Other compounds exhibited considerable activity, such as compounds 9 (IC50 3.5 and 19.0 μM), 10 (IC50 12.6 μM), and 11 (IC50 10.3 μM) against the three cancer cell lines HCT116, MCF-7 and K562, respectively.


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