Table 1.
Antiproliferative activity and effect on tubulin assembly.
| Compound | IC50 (μM) a | Tubulin Assay | |||||
|---|---|---|---|---|---|---|---|
| A549 | MDA-MB-231 | KB | KB-VIN | MCF-7 | ITAd (μM) | ICBe (%) | |
| 1 | 6.9 ± 0.1 | 5.9 ± 0.0 | 5.5 ± 0.0 | 7.4 ± 0.3 | 7.2 ± 0.4 | NTb | NT |
| 2 | >40 | >40 | >40 | >40 | >40 | NAc | NA |
| 3 | 0.6 ± 0.0 | 0.9 ± 0.0 | 0.6 ± 0.0 | 0.6 ± 0.1 | 2.2 ± 0.2 | NT | NT |
| 4 | 5.6 ± 0.0 | 8.2 ± 0.8 | 5.8 ± 0.3 | 6.3 ± 0.2 | 10.0 ± 0.9 | NT | NT |
| 5 | >40 | >40 | >40 | >40 | >40 | NA | NA |
| 6 | 0.5 ± 0.0 | 0.8 ± 0.0 | 0.5 ± 0.0 | 0.5 ± 0.0 | 0.8 ± 0.0 | 0.7 ± 0.0 | 54 ± 0.8 |
| 7 | 5.6 ± 0.1 | 9.8 ± 0.9 | 5.4 ± 0.3 | 6.1 ± 0.4 | 10.8 ± 0.8 | 4.6 ± 0.1 | 35 ± 1 |
| 8 | 27.7 ± 0.1 | 34.5 ± 0.2 | >40 | >40 | >40 | NA | NA |
| 9 | 0.8 ± 0.0 | 6.0 ± 0.8 | 0.9 ± 0.0 | 0.7 ± 0.0 | 10.2 ± 0.5 | NT | NT |
| 10 | >40 | >40 | >40 | >40 | >40 | NA | NA |
| 11 | >40 | >40 | 26.5 ± 2.5 | >40 | >40 | NA | NA |
| 12 | 5.2 ± 0.1 | 6.8 ± 1.1 | 5.4 ± 0.4 | 5.8 ± 0.1 | 8.2 ± 0.9 | NT | NT |
| 13 | 0.7 ± 0.1 | 0.9 ± 0.0 | 0.7 ± 0.0 | 0.7 ± 0.0 | 6.7 ± 0.1 | NT | NT |
| 14 | >40 | >40 | >40 | >40 | >40 | NA | NA |
| VIN (nM) | 22.9 ± 2.4 | 32.0 ± 0.5 | 4.4 ± 0.1 | 2479.2 ± 28.2 | 7.3 ± 0.2 | NT | NT |
| PXL (nM) | 4.5 ± 0.9 | 7.0 ± 0.9 | 3.7 ± 1.1 | 2357.7 ± 59.5 | 8.8 ± 1.0 | NT | NT |
| CA-4 (nM) | 5.5 ± 0.1 | 8.2 ± 0.5 | 3.6 ± 0.1 | 3.8 ± 0.1 | 487.4 ± 11 | 0.7 ± 0.0 | 100 ± 0.4 |
a Antiproliferative activity as IC50 values for each cell line, the concentration of compound that caused a 50% reduction relative to untreated cells determined by the SRB assay. b NT, not tested. c NA, not active (IC50 > 40 µM). d Inhibition of purified tubulin assembly, EC50 (µM) values of 50% inhibition (ITA). e Percent inhibition of 5 μM [3H] colchicine binding to 1 μM tubulin in the presence of 5 μM test compound (ICB).