Table 3.
Inhibition of tubulin polymerization and colchicine binding by compounds 1, 2a–c, 2f–h and 2j
| Compound | Tubulin assemblya,c IC50 ± SD (µM) |
Colchicine bindingb,c % ± SD |
|---|---|---|
| 2a | 1.9 ± 0.02 | 52 ± 0.9 |
| 2b | 3.1 ± 0.2 | 46 ± 0.9 |
| 2c | 0.74 ± 0.06 | 84 ± 5 |
| 2f | >20 | n.d. |
| 2g | 10 ± 0.7 | n.d. |
| 2h | >20 | n.d. |
| 2j | 16 ± 1 | n.d. |
| 1 | 2.0 ± 0.06 | 52 ± 4 |
n.d. = not determined.
Inhibition of tubulin polymerization. Tubulin was at 10 µM.
Inhibition of [3H]colchicine binding. Tubulin, colchicine and tested compound were at 1, 5 and 5 µM, respectively.
Values are mean ± SD of four separate experiments.