Background:
Quinolones are a significant group of nitrogen heterocyclic compounds that exist in therapeutic
agents, alkaloids, and synthetic small molecules that have important biological activities. A wide range of
quinolones have been used as antituberculosis, antibacterial, anti-malarial, antifungal, anticonvulsant, anticancer
agents and urease inhibitors.
Methods:
Ethyl 3,3-disubstituted-2-cyano propionates containing hybride quinolones derivatives were synthesized
by the reaction of 1-amino-7-hydroxy-4-methylquinolin-2(1H)-one and its dibromo derivative with α, β-unsaturated
carbonyl in ethanol.
Results:
A novel series of hybrid 2-quinolone derivatives was designed and synthesized. The compounds structures
were confirmed using different spectroscopic methods and elemental analysis. The cytotoxic activities of all the
compounds were assessed against HepG2 cell line in comparison with doxorubicin as a standard drug.
Conclusion:
Most compounds revealed superior anti-proliferative activity than the standard. Compound 4b, is the
most active compound (IC50 = 0.39mM) compared with doxorubicin (IC50 = 9.23mM). DNA flow cytometric analysis
of compound 4b showed cell cycle arrest at G2/M phase with a concomitant increase of cells in apoptotic phase.
Dual annexin-V/ propidium iodide staining assay of compound 4b revealed that the selected candidate increased the
apoptosis of HepG-2 cells more than control.
Corrigendum to “Design and synthesis of novel isatin-based derivatives targeting cell cycle checkpoint pathways as potential anticancer agents” [Bioorg. Chem. 105 (2020) 104366]
