Table 3.
Kinase inhibitory activity a,b of the thiazolo[5,4-f]quinazoline series 11a–c, 12a–n, 13a–h, 14a–e, 15a–c.
| Compounds | CDK5/p25 | CK1δ/ε | CLK1 | DYRK1A | GSK-3α/β |
|---|---|---|---|---|---|
| 11a | >10 | >10 | 1.1 | 3.3 | 3.3 |
| 11b | >10 | >10 | 4.1 | 7.8 | ≥10 |
| 11c | >10 | >10 | 1.3 | 7.7 | 1.2 |
| 12a | 3.9 | >10 | 0.031 | 0.091 | 0.082 |
| 12b | >10 | >10 | 0.51 | 0.39 | 1.2 |
| 12c | >10 | >10 | 0.21 | 0.32 | 0.12 |
| 12d | 3.0 | 5.4 | 0.16 | 0.14 | 0.041 |
| 12e | 4.9 | >10 | 0.29 | 0.072 | 0.028 |
| 12f | >10 | >10 | 0.091 | 0.13 | 0.16 |
| 12g | 1.8 | >10 | 0.38 | 0.17 | 0.030 |
| 12h | >10 | >10 | 0.99 | 0.5 | 0.3 |
| 12i | >10 | >10 | 1.8 | 1.0 | 1.8 |
| 12j | >10 | >10 | 0.69 | 0.2 | 1.2 |
| 12k | >10 | >10 | 0.88 | 0.38 | 0.51 |
| 12l | >10 | >10 | 7.9 | 3.0 | 1.20 |
| 12m | >10 | >10 | >10 | >10 | ≥10 |
| 12n | >10 | >10 | 0.080 | 0.18 | 1.7 |
| 13a | >10 | >10 | 0.06 | 0.06 | 0.1 |
| 13b | >10 | >10 | 0.59 | 0.29 | 0.69 |
| 13c | >10 | >10 | 0.48 | 0.16 | 0.11 |
| 13d | >10 | >10 | 0.27 | 0.13 | 0.057 |
| 13e | >10 | >10 | 0.32 | 0.062 | 0.028 |
| 13f | >10 | >10 | 0.071 | 0.059 | 0.071 |
| 13g | >10 | >10 | 1.30 | 0.28 | 0.083 |
| 13h | >10 | >10 | 1.40 | 0.21 | 0.15 |
| 14a | >10 | >10 | 0.1 | 0.21 | 0.2 |
| 14b | >10 | >10 | 1.9 | 0.82 | 1.2 |
| 14c | >10 | >10 | 0.49 | 0.37 | 0.17 |
| 14d | >10 | >10 | 0.34 | 0.37 | 0.17 |
| 14e | >10 | >10 | 0.78 | 0.23 | 0.029 |
| 15a | >10 | >10 | 0.043 | 0.42 | 0.42 |
| 15b | >10 | >10 | 2.1 | 3.9 | 2.5 |
| 15c | >10 | >10 | 1.2 | 0.95 | 0.27 |
| Harmine | >10 | 1.5 | 0.026 | 0.029 | >10 |
a IC50 values are reported in μM. The most significant results are presented in bold; b Kinases activities were assayed in triplicate. Typically, the standard deviation of single data points was <10%.