Table 2.
Inhibition of tubulin polymerization and colchicine binding by synthesized compounds and CA-4.
| Compound | Inhibition of tubulin assemblya IC50 (µM)± SD |
Inhibition of colchicine bindingb % Inhibition ± SD |
||
|---|---|---|---|---|
| 50 µM | 5 µM | 1 µM | ||
| 3a | > 40 | 13 ± 5 | - | - |
| 3b | > 40 | 15 ± 5 | - | - |
| 3c | > 40 | 11 ± 2 | - | - |
| 3d | > 40 | 26 ± 5 | - | - |
| 3e | 17 ± 1 | 50 ± 4 | 11 ± 4 | - |
| 3f | > 40 | 11 ± 1 | - | - |
| 3g | > 40 | 14 ± 5 | - | - |
| 3h | > 40 | 12 ± 4 | - | - |
| 3i | > 40 | 13 ± 4 | - | - |
| 3j | > 40 | 23 ± 2 | - | - |
| 3k | > 40 | 13 ± 0.2 | - | - |
| CA-4 | 1.3 ± 0.07 | 98 ± 0.8 | 88 ± 0.3 | |
a
Tubulin was at 10 µM.
b
Tubulin and colchicine were at 1 and 5 µM concentrations, respectively.