| dc.description.abstract | The cytotoxic activities of the compounds were determined by the 3‐(4,
5‐dimethylthiazolyl‐2)‐2,5‐diphenyltetrazolium bromide (MTT) method in human
breast cancer (MCF‐7), human cervical cancer (HeLa), and mouse fibroblast (L929)
cell lines. The compounds MAAS‐5 and four modified the supercoiled tertiary
structure of pBR322 plasmid DNA. MAAS‐5 showed the highest cytotoxic activity in
HeLa, MCF‐7, and L929 cells with IC50 values of 16.76 ± 3.22, 28.83 ± 5.61, and
2.18 ± 1.22 μM, respectively. MAAS‐3 was found to have almost the lowest
cytotoxic activities with the IC50 values of 93.17 ± 9.28, 181.07 ± 11.54, and
16.86 ± 6.42 μM in HeLa, MCF‐7, and L929 cells respectively at 24 h. Moreover, the
antiepileptic potentials of these compounds were investigated in this study. To this
end, the effect of newly synthesized Schiff base derivatives on the enzyme activities
of carbonic anhydrase I and II isozymes (human carbonic anhydrase [hCA] I and hCA
II) was evaluated spectrophotometrically. The target compounds demonstrated
high inhibitory activities compared with standard inhibitors with Ki values in the
range of 4.54 ± 0.86–15.46 ± 8.65 nM for hCA I (Ki value for standard inhibitor =
12.08 ± 2.00 nM), 1.09 ± 0.32–29.94 ± 0.82 nM for hCA II (Ki value for standard
inhibitor = 18.22 ± 4.90 nM). Finally, the activities of the compounds were compared
with the Gaussian programme in the B3lyp, HF, M062X base sets with 6‐31++G (d,p)
levels. In addition, the activities of five compounds against various breast cancer
proteins and hCA I and II were compared with molecular docking calculations. | tr |
