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. Author manuscript; available in PMC: 2023 Dec 5.
Published in final edited form as: ChemMedChem. 2022 Oct 13;17(23):e202200408. doi: 10.1002/cmdc.202200408

Table 5.

Steroid sulfatase inhibition of difluoromethoxy-substituted estratriene sulfamate derivatives in JEG-3 human choriocarcinoma assays in vitro.[a]

graphic file with name nihms-1838934-t0011.jpg

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
[a]

Results are IC50 values in nM and are the mean of three determinations. N.D. not determined.