Table 2.
Inhibition of tubulin polymerization and colchicine binding by 1–29.
| Comp. No. | Tubulin polymerization inhibition
|
Inhibition of colchicine binding (% ± SD)
|
|
|---|---|---|---|
| IC50 (μM ± SD) | 50 μM | 5 μM | |
| 1 | 2.9 ± 0.3 | 39 ± 5 | 24 ± 0.8 |
| 2 | 5.2 ± 0.2 | 38 ± 1 | 9.3 ± 3 |
| 3 | 6.5 ± 0.08 | 14 ± 5 | 7.0 ± 4 |
| 4 | >20 | / | / |
| 5 | >20 | / | / |
| 6 | 9.7 ± 1 | 25 ± 2 | 3.1 ± 3 |
| 7 | >20 | / | / |
| 8 | 11 ± 2 | 14 ± 0.8 | 9.6 ± 5 |
| 9 | 8 ± 0.08 | 19 ± 4 | 12 ± 0.01 |
| 10 | >20 | / | / |
| 11 | >20 | / | / |
| 12 | >20 | / | / |
| 13 | >20 | / | / |
| 14 | >20 | / | / |
| 15 | >20 | / | / |
| 16 | >20 | / | / |
| 17 | 11 ± 0.07 | 13 ± 2 | 8.9 ± 2 |
| 18 | >20 | / | / |
| 19 | >20 | / | / |
| 20 | 18 ± 0.9 | / | / |
| 21 | 11 ± 0.1 | 20 ± 5 | 2.7 ± 4 |
| 22 | >20 | / | / |
| 23 | 3.5 ± 0.3 | 31 ± 4 | 11 ± 3 |
| 24 | 11 ± 0.6 | 19 ± 0.8 | 2.8 ± 1 |
| 25 | 10 ± 2 | 20 ± 5 | 0.3 ± 2 |
| 26 | 8.6 ± 0.5 | 28 ± 4 | 6.2 ± 3 |
| 27 | 7.8 ± 1 | 24 ± 2 | 5.9 ± 5 |
| 28 | >20 | / | / |
| 29 | >20 | / | / |
| Combretastatin A-4 | 1.2 ± 0.007 | / | 99 ± 0.7 |