Table 4.
Inhibition of Tubulin Assembly and Inhibition of Colchicine Binding.
Compd | Inhibition of tubulin assembly IC50 ± SD (µM) |
Inhibition of colchicine binding (% inhibition ± SD) at 5 µM |
---|---|---|
6 | 1.4 ± 0.007 | 84 ± 0.5 |
14 | 1.7 ± 0.2 | 76 ± 3 |
15 | 1.7 ± 0.07 | 82 ± 1 |
1 | 2.6 ± 0.05 | 70 ± 2 |
CA-4 | 1.0 ± 0.09 | 99 ± 0.2 |
Inhibition of tubulin assembly was performed as described previously,26 with tubulin at 10 µM (1.0 mg/mL) and varying concentrations of potential inhibitors. Extent of assembly at 20 min was the parameter measured. The CA-4 control is performed twice a year, and IC50 values obtained range from 1 to 1.2 µM. The most recent value is shown in the table. Inhibition of colchicine binding was performed as described previously,27 with tubulin at 1.0 µM and both [3H]colchicine and potential inhibitor at 5.0 µM. Incubation was for 10 min at 37 °C.