Table 3.
Inhibition of tubulin polymerization and colchicine binding by compounds 4a, 4c–d, 4i, 4k, 4o and CA-4.
| Compound | Tubulin assemblya | Colchicine bindingb |
|---|---|---|
| IC50±SD (μM) | %±SD | |
| 4a | 1.3 ± 0.2 | 57 ± 5 |
| 4c | 1.2 ± 0.1 | 62 ± 1 |
| 4d | 2.2 ± 0.3 | 41 ± 5 |
| 4i | 1.2 ± 0.0 | 70 ± 3 |
| 4k | 2.0 ± 0.3 | 46 ± 4 |
| 4o | 2.7 ± 0.0 | 30 ± 3 |
| CA-4 (1) | 1.1 ± 0.1 | 99 ± 3 |
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.