Table 2:
Bioassays with diaryl disulfides
|
IC50 μM ± SD |
Inhibition of colchicine bindingc % Inhibition ± SD | ||
|---|---|---|---|---|
| Inhibition of tubulin assemblya (relative to CSA4) | Inhibition of MCF-7 cell growthb | |||
|
|
||||
| R = ortho (o), meta (m), para (p) - F, Cl, Br | 5 μM inhibitor | 50 μM inhibitor | ||
|
| ||||
| CA-4 | 0.54 ± 0.06 | 0.039 ± 0.006 | 98 ± 1 | 100 ± 0.04 |
| (2a) o-F | 2.4 ± 0.3 (4.4) | > 10 | 0 ± 4 | 53 ± 5 |
| (2b) m-F | 4.8 ± 0.1 (8.9) | > 10 | 1.4 ± 4 | 12 ± 2 |
| (2c) p-F | 1.9 ± 0.06 (3.5) | > 10 | 2.6 ± 4 | 17 ± 4 |
| (2d) o-Cl | 1.4 ± 0.2 (2.6) | > 10 | 15 ± 5 | 36 ± 2 |
| (2e) m-Cl | 3.1 ± 0.4 (5.7) | > 10 | 12 ± 2 | 18 ± 5 |
| (2f) p-Cl | 4.6 ± 0.7 (8.5) | > 10 | 9.8 ± 2 | 0 ± 4 |
| (2g) o-Br | 1.2 ± 0.1 (2.2) | > 10 | 27 ± 3 | 34 ± 4 |
| (2h) m-Br | 4.0 ±0.5 (7.4) | > 10 | 6.6 ± 5 | 17 ± 4 |
| (2i) p-Br | 5.1 ± 0.5 (9.4) | > 10 | 11 ± 0.3 | 0 ± 2 |
a
Averages of three independent experiments.
b
Single determination, except for CA-4.
c
Averages of two independent experiments.