Nine novel hydrazone derivatives (4a-i) incorporating pyridine and isatin moieties were synthesized through one-pot, four-component heterocyclic condensation reactions. The structures of all new compounds (2a-e, 3a, 3c-e, and 4a-e) were identified by 1 H nuclear magnetic resonance (NMR), 13 C NMR, and Fouriertransform infrared spectroscopic techniques and elemental analysis. Cell viability assays for the tested hydrazone derivatives were performed and the log IC 50 values of the compounds were calculated after a 24-h treatment. All hydrazide derivatives tested showed a promising antitumor activity against A-2780 cells as compared with the standard drug docetaxel with a log IC 50 value of 0.2200 μM (p < .05). Seven of the examined compounds (4b-e, 4g-i) showed high cytotoxic activity against A-2780 cells as compared with the standard drug docetaxel. Whereas the log IC 50 of docetaxel was 0.2200 μM for A-2780 cells at 24 h, the IC 50 values of these compounds were −0.4987, −0.4044, −0.8138, −0.3868, −0.6954, −0.4751, and 0.1809 μM, respectively. Three of the compounds, 4b, 4d, and 4i, showed high cytotoxic activity against MCF-7 cells as compared with docetaxel (p < .05). Whereas the log IC 50 of docetaxel was 0.2400 μM for MCF-7 cells at 24 h, the log IC 50 values of compounds 4b, 4d, and 4i were −0.1293, −0.1700, and 0.2459 μM, respectively.anticancer activity, hydrazone derivatives, isatin derivatives, pyridine derivatives
| INTRODUCTIONDue to the increase in cancer incidence, scientific research on cancer morbidity and mortality and improvement in the quality of life of cancer patients is increasing rapidly. Cancer is a serious health concern in all societies, regardless of wealth or social status.