Table 5.
Steroid sulfatase inhibition of difluoromethoxy-substituted estratriene sulfamate derivatives in JEG-3 human choriocarcinoma assays in vitro.[a]
| |||||
|---|---|---|---|---|---|
|
| |||||
| Cpd | R1 | R2 | R3, R4 | Cell lysate | Whole cells |
|
| |||||
| 4 | SO2NH2 | OCH3 | H, OSO2NH2 | 99 | 4.2 |
| 10 | SO2NH2 | OCF2H | H, OSO2NH2 | 44 | 3.7 |
| 11 | H | OCF2H | H, OSO2NH2 | >5000 | N.D. |
| 12 | SO2NH2 | OCF2H | H, OH | 75 | 18.6 |
| 16 | SO2NH2 | OCF2H | =O | 56 | 5.6 |
| 23 | SO2NH2 | CF2H | =O | 19 | 0.055 |
| 25 | SO2NH2 | H | =O | 79 | 0.118 |
Results are IC50 values in nM and are the mean of three determinations. N.D. not determined.