Table 1.
Biological activities of compounds 7-20 (μM)
| Compound | Cdc25Ba | MKP-1a | MKP-3a | A2780b |
|---|---|---|---|---|
| Adociaquinone B | 0.08/0.11 | 1.10 | 1.53 | 26 ± 0.06 |
| 7 | 9.53 | 21.8 | >50 | 0.75 ± 0.03 |
| 8 | 22.3 | > 50 | 49.9 | 1.4 ± 0.07 |
| 9 | 2.3 | 38.7 | > 50 | 6.9 ± 0.1 |
| 10 | > 50 | > 50 | > 50 | 7.8 ± 0.4 |
| 11 | 2.76 | 8.45 | 19.8 | 2.3 ± 0.03 |
| 12 | 9.51 | > 50 | > 50 | 0.58 ± 0.45 |
| 13 | 3.38 | 24.0 | 20.5 | 2.6 ± 0.06 |
| 14 | 1.98 | 13.0 | 12.4 | 1.4 ± 0.05 |
| 15 | 1.00 | 9.37 | 6.90 | 0.08 ± 0.001 |
| 16 | 0.94 | 17.8 | 42.6 | 4.3 ± 2.3 |
| 17 | 0.88 | 33.8 | > 50 | 2.1 ± 0.02 |
| 18 | > 50 | > 50 | > 50 | 64 ± 1.2 |
| 19 | > 50 | > 50 | > 50 | * |
| 20 | 0.27 | 0.82 | 1.35 | 0.37 ± 0.01 |
a
IC50 values (μM) for activity against the catalytic domain of Cdc25B. The data for adociaquinone B are for activity against the catalytic domain (0.11) and full length Cdc25B (0.08)
b
Antiproliferative activity (IC50 μM); growth of the A2780 human ovarian cell line according to the procedure described.29,4,3,44 with paclitaxel (IC50 23.4 nM) as the positive control. All compounds were tested in triplicate in this assay.
*
The fluorescence reading was not indicative of the true biological activity of 19. The fluorescence reading indicated that 19 was not active, but microscopic analysis clearly showed that significant inhibition of the growth of A2780 cells occurred.