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Comparative effects on in vivo estrogen antagonism for various basic side chain modifications in the raloxifene nucleus
| Compound | R | In Vivo estrogen antagonism, maximal percent inhibition (Uterine wt/body wt) |
|---|---|---|
| Tamoxifen | 48* | |
| 1 | 91* | |
| 1g | 81* | |
| 1h | 3.8 | |
| 1i | 10 | |
| 1j | 38* | |
| 1k | 36* |
Statistical significance relative to ethynyl estradiol-treated control (P ≤ 0.05).
