Table 2.
Inhibition of tubulin polymerization and colchicine binding by compounds 2a, 4f-g, 5, and CA-4
Compound | Tubulin assemblya IC50 ± SD (μM) |
Colchicine bindingb ±SD (%) |
|
---|---|---|---|
1 μM inhibitor | 5 μM inhibitor | ||
n.d., not done. | |||
2a | 1.9 ± 0.1 | 25 ± 2 | 71 ± 1 |
4f | 0.6 ± 0.02 | 71 ± 0.6 | 84 ± 3 |
4g | 0.6 ± 0.03 | 67 ± 2 | 82 ± 2 |
5 | 5.4 ± 0.4 | n.d. | 27 ± 0.1 |
CA-4 (1) | 1.2 ± 0.1 | 90 ± 1 | 99 ± 0.7 |
Inhibition of tubulin polymerization. Tubulin was at 10 μM.
Inhibition of [3H]colchicine binding. Tubulin and colchicine were at 1 and 5 μM, respectively, and the tested compound was at the indicated concentration.