Table 5.
Effects of the (5Z) 2-amino-5-arylidene-1,3-thiazol-4(5H)-one derivatives 5a–x on the catalytic activity of four purified protein kinases a.
| Compound | DYRK1A | CK1 | CDK5/p25 | GSK3α/β |
|---|---|---|---|---|
| 5a | 0.63 | - | - | 7.4 |
| 5b | >10 | - | - | - |
| 5c | - | - | - | - |
| 5d | >10 | - | - | - |
| 5e | 1.8 | - | - | ≤8.8 |
| 5f | 2.3 | - | - | - |
| 5g | 0.4 | - | - | ≥10 |
| 5h | - | - | - | - |
| 5i | 0.053 | - | - | 7.4 |
| 5j | ≥10 | - | - | - |
| 5k | 1.6 | - | - | - |
| 5l | 1.8 | - | - | >10 |
| 5m | 0.6 | >10 | - | ≥10 |
| 5n | 0.070 | >10 | - | 5.3 |
| 5o | 0.090 | ≥10 | - | 4.7 |
| 5p | 0.94 | ≥10 | - | >10 |
| 5q | 0.17 | - | - | 3.7 |
| 5r | 0.61 | - | - | - |
| 5s | 0.033 | - | - | ≤10 |
| 5t | >10 | - | - | >10 |
| 5u | 0.9 | - | - | >10 |
| 5v | 9.0 | >10 | >10 | >10 |
| 5w | 0.12 | - | - | - |
| 5x | 0.27 | - | - | - |
| Harmine | 0.029 | 1.5 | >10 | >10 |
| (R)-Roscovitine | 11 | 2.3 | 0.2 | 130 |
a Compounds were tested at various concentrations on each kinase as described in Experimental Section. IC50 values, calculated from the dose-response curves, are reported in μM. -, inactive at the highest concentration tested (10 μM); >10, inhibitory, but IC50 > 10 μM.