Table 2.
Inhibition of tubulin polymerization and colchicine binding by compounds 4b, 4d, 4p–r, 4t–w and CA4
| Compound | Tubulin assemblya IC50 ± SD (μM) | Colchicine bindingb % ± SD |
|---|---|---|
| 4b | 1.1 ± 0.1 | 76 ± 2 |
| 4d | 0.70 ± 0.08 | 79 ± 0 |
| 4p | 1.8 ± 0.2 | 66 ± 0 |
| 4q | 1.2 ± 0.1 | 65 ± 0 |
| 4r | 0.55 ± 0.03 | 97 ± 1 |
| 4t | 0.43 ± 0.06 | 96 ± 1 |
| 4u | 6.9 ± 0.8 | n.d. |
| 4v | 0.57 ± 0.03 | 85 ± 1 |
| 4w | 1.1 ± 0.1 | 69 ± 3 |
| CA4 (1) | 1.0 ± 0.1 | 99 ± 2 |
n.d.: not determined.
a
Inhibition of tubulin polymerization. Tubulin was at 10 μM.
b
Inhibition of [3H]colchicine binding. Tubulin, colchicine and tested compound were at 1, 5 and 5 μM,respectively.