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Updated: May 27, 2025
Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Synthesis, Characterization and Preliminary Screening of New N-Substituted -8-Methyl-4-Hydroxy-2-Quinolone
Dania Altaher1, Hiba Zalloum2, Kamal Sweidan1
1Department of Chemistry, The University of Jordan, Amman, 11942, Jordan.
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 characterization using 1D-NMR, 2D-NMR, and IR techniques.
Methods:
The final products contain amide, hydroxyl, and aromatic functional groups that usually 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.
