Table 3.
Examples of nonsteroidal STS inhibitors containing phosphorus moieties 33–46.
| General structure | Substituents | Example | STS inhibitory effects | Ref. [year] |
|---|---|---|---|---|
 |
R = Cl, NH2, OCH3 or OCH2CH3; X = O or S; n = 1, 2, or 3. |
 |
IC50 value of 21.5 µM (in an assay with purified enzyme) |
78 [2014] |
 |
IC50 value of 13.3 µM (in an assay with purified enzyme) |
79 [2015] |
||
 |
R = Cl, OH, NH2 or OCH3; n = 1, 2, or 3. |
 |
IC50 value of 860 nM (in an assay with purified enzyme). |
80 [2015] |
 |
IC50 value 7.76 µM (in an assay with purified enzyme). |
|||
 |
IC50 value of 6.77 µM (in an assay with purified enzyme) |
|||
 |
R1 = Cl, OH, NH2, OCH3 or OCH2CH3; R2 = H or CH2CH3; X = O or S. |
 |
IC50 value of 46.8 µM (in an assay with purified enzyme) |
81 [2015] |
 |
R1 = Cl, OH, or OCH3; R2 = H, F, CH3 or CF3; X = O or S. |
 |
IC50 value of 29.0 µM (in an assay with purified enzyme) |
82 [2015] |
 |
R = Cl, OH, NH2 or OCH3. |  |
IC50 value of 22.1 µM (in an assay with purified enzyme) |
81 [2015] |
 |
R1 = H, F, CH3 or CF3; R2 = Cl, OH, or OCH3. |
 |
IC50 value 3.2 µM (in an assay with purified enzyme) |
82 [2015] |
 |
R = OH, NH2 or OCH3; X = O or S; n = 10, 11, or 12. |
 |
IC50 value of 0.39 µM (in an assay with purified enzyme) |
83 [2015] |
 |
IC50 value of 1.31 µM (in an assay with purified enzyme) |
|||
 |
R1 = CH3, CH2CH3, iso-propyl, n-butyl, Ph, CH2Ph; R2 = H or CH3; X = O or S. |
 |
IC50 value of 190 nM (in an assay with purified enzyme) |
84 [2016] |
 |
IC50 value of 240 nM (in an assay with purified enzyme) |
|||
 |
IC50 value of 200 nM (in an assay with purified enzyme) |
85 [2019] |