TABLE 4
Inhibition of human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity by raloxifene and structural analogs
Values for IC50 are means ± S.E.
Compound | R1 | R2 | R3 | R4 | IC50 |
|---|---|---|---|---|---|
| μM | |||||
| 1 | OCH3 | OCH3 | H | X | 8.0 ± 5.4 |
| 2 | OH | OH | H | Y | 0.0070 ± 0.0000 |
| 3 | OH | OH | H | H | 0.24 ± 0.07 |
| 4 | OH | H | OH | X | 0.051 ± 0.004 |
| 5 | CF3 | OH | H | X | 0.089 ± 0.020 |
| Raloxifene | OH | OH | H | X | 0.0057 ± 0.0004 |
