Table 1.
Inhibition of Tubulin Polymerization and Colchicine Binding
| compound | inhibition of tubulin polymerizationa IC50 | inhibition of colchicine bindingb % inhibition ± SD | |
|---|---|---|---|
| (μM)±SD | 1 μM | 5 μM | |
| 29 (CA1)c | 1.9 | NDd | 99.6±0.7 |
| 42 (CA4) | 0.64±0.01 | 84±2 | 97±0.7 |
| 20 | 0.84±0.1 | 50±5 | 84±1 |
| 21 | 0.82±0.04 | 72±4 | 94± 0.7 |
| 22 | >20 | ||
| 23 | >20 | ||
| 24 | 12±1 | ||
| 25 | >20 | ||
| 26 | 9.5±0.9 | ||
| 35 | 1.7±0.2 | 25±3 | |
| 36 | >20 | ||
| 37 | 1.7±0.01 | 53±3 | 92±0.5 |
| 38 | 0.84±0.1 | 34±3 | 90±0.7 |
| 39 | 4.3±0.4 | 58±4 | |
| 40 | 6.2±0.3 | 72±3 | |
| 41 | 1.3±0.08 | 43±4 | |
| 43 | >20 | 26±1 | |
| 44 | >20 | 15±5 | |
| 45 | >20 | 33±3 | |