Table 1.
Compound | R | R′ | ER RBA | MCF-7 Inhib. IC50 (nM) |
---|---|---|---|---|
17β-estradiol | 1.00 | NA | ||
4-OH Tam | 0.36 | 0.5 | ||
Raloxifene (1) | 6-OH | OH | 0.34 | 0.2 |
1a | None | OH | .003 | 35 |
1b | 6-OMe | OH | .008 | 250 |
1c | 7-OH | OH | .020 | 300 |
1d | 5-OH | OH | 0.1 | 100 |
1e | 6-OH | H | .062 | 2.5 |
1f | None | H | .002 | >100 |
NA, not applicable.