Table 3:
Bioassays with diaryl thiosulfonates
|
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 μinhibitor | 50 μM inhibitor | ||
|
| ||||
| CA-4 | 1.3 ± 0.1 | 0.021 ± 0.004 | 98 ± 1 | 100 ± 0.04 |
| (3a) o-F | 5.5 ± 0.1 (4.2) | > 10 | 0 | 75 ± 5 |
| (3b) m-F | 3.1 ± 0.2 (2.4) | > 10 | 8.9 ± 0.9 | 97 ± 0.1 |
| (3c) p-F | 1.2 ± 0.06 (0.92) | 7.5 ± 0d | 52 ± 5 | 100 ± 0.3 |
| (3d) o-Cl | 6.3 ± 0.3 (4.8) | > 10 | 12 ± 2 | 31 ± 4 |
| (3e) m-Cl | 4.7 ± 0.04 (3.6) | > 10 | 93 ± 1 | |
| (3f) p-Cl | 9.1 ± 0.9 (7.0) | 10 ± 0d | 0 | 75 ± 2 |
| (3g) o-Br | 1.3 ± 0.06 (1.0) | > 10 | 18 ± 5 | 90 ± 0.3 |
| (3h) m-Br | 3.3 ± 0.04 (2.5) | > 10 | 20 ± 1 | 99 ± 1 |
| (3i) p-Br | 4.2 ± 0.2 (3.2) | > 10 | 6.6 ± 4 | 80 ± 2 |
a
Averages of three independent experiments.
b
Single determination, except for CA-4, 3c and 3f.
c
Averages of two independent experiments.
d
The same value was obtained twice.