Table 5.
Activity of selected THIQs as inhibitors of tubulin polymerisation and [3H]colchicine binding to tubulin.
| Compd | Tubulin assembly IC50 [μM][a] |
Colchicine binding Inhibition at 5 μM inhibitor [%][a] |
|---|---|---|
| CA-4 | 1.2 ±0.1 | 98 ±0.7 |
| 3a | > 20 (no activity)[b] | 4.1 ±2 |
| 4a | > 20 (partial activity)[b] | 10±0.9 |
| 4b | 2.5 ±0.3 | 49 ±0.5 |
| 12e | 5.6 ±0.7 | 32 ±3 |
| 12f | 2.4 ±0.4 | 45 ±0.6 |
| 12j[c] | 2.4 ±0.2 | 50 ±4 |
| 15 | 1.8 ±0.04 | 78±2 |
| 20b | 1.6 ±0.1 | 73±3 |
[a]
Data are the mean ±SD of at least two determinations.
[b]
Compound 4a inhibits tubulin assembly at 20 μM while 3a is inactive at this concentration.
[c]
Compound 12j is a racemic mixture. Data for CA-4, 3a and 4a,b are taken from the literature [12].