In vitro enzymatic inhibitory activity of the three promising cytotoxic compounds 1a (pyridine-thiourea) precursor, 8a (5-acetyl-thiazolidin-4-one) derivative and 13a (5-(p-tolyldiazenyl-2,3-dihydrothiazole)) derivative against CDK2/cyclin A and GSK3βa.
| Cpd | IC50 (mean ± SEM) (μg mL−1) | |
|---|---|---|
| CDK2/cyclin A | GSK3β | |
| 1a | 3.25 | 0.438 |
| 8a | 0.675 | 0.134 |
| 13a | 0.396 | 0.118 |
| Roscovitine | 0.88 | — |
| CHIR-99021 | — | 0.07 |
a
IC50: compound concentration necessary to inhibit the enzyme activity by 50%; SEM: standard error of the mean; each value is the mean of three values; (—) not detected.