Abstract
In this study, twenty new anthranilic acid hydrazones 6-9 (a-e) were synthesizedand their structures were characterized by Fourier-transform Infrared (FTIR), Nuclear Magnetic Resonance (1H NMR - 13C NMR), and High-resolution Mass Spectroscopy (HRMS). The inhibitory effects of thecompounds against COX-II were evaluated. IC50 values of the compounds were found in the range of >200 - 0.32 µM and compounds 6e, 8d, 8e, 9b, 9c, and 9e were determined to be the most effective inhibitors. Cytotoxic effects of the most potent compounds were investigated against human hepatoblastoma (Hep-G2) and human healthy embryonic kidney (Hek-293) cell lines. Doxorubicin (IC50: 8.68 ± 0.16 µM for Hep-G2, 55.29 ± 0.56 µM for Hek-293) was used as standard.8e is the most active compound, with low IC50against Hep-G2 (4.80 ± 0.04 µM), high against Hek-293 (159.30 ± 3.12), and high selectivity (33.15). Finally, molecular docking and dynamics studies were performed to understand ligand-protein interactions between the most potent compounds and COX II, Epidermal Growth Factor Receptor (EGFR), and Transforming Growth Factor beta II (TGF-βII). The docking scores were calculated in the range of -10.609 - -6.705 kcal/mol for COX-II, -8.652 - -7.743 kcal/mol for EGFR and -10.708 - -8.596 kcal/mol for TGF-βII.
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