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In this study, some new thiosemicarbazide and their corresponding 1,3,4-thiadiazole derivatives containing pyridine nuclei were synthesized. Their structures were established based on FT-IR, ¹HNMR , ¹³CNMR , 2D-NMR (HSQC) spectral data and elemental analysis. The MCF-7 and NIH3T3 cells were used to test the compound's anticancer effects. Among the compounds; 4a, 4b, 4d and 4g showed the most potent cytotoxic activity against MCF-7 at IC₅₀ of 3.102±0.096 μM, 8.737±0.103 μM, 11.190±0.088 μM and 12.630±0.101 μM, respectively.Their inhibitory activity was assessed against the in vitro aromatase enzyme. Compounds 4a, 4b, 4d and 4g exhibited the promising aromatase inhibition activity with IC₅₀ value of 0.027±0.002 µM, 0.068±0.005 µM, 1.456±0.009 µM and 3.316±0.001 µM, respectively (the standard drug letrazole has an IC₅₀ value of 0.023±0.002 μM). The molecular docking studies were …