Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 49, Issue 26, Pages 7596-7599Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm061101w
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A novel, N-aryl-bicyclohydantoin selective androgen receptor modulator scaffold was discovered through structure-guided modifications of androgen receptor antagonists. A prototype compound (7R,7aS)-10b from this series is a potent and highly tissue-selective agonist of the androgen receptor. After oral dosing in a rat atrophied levator ani muscle model, (7R,7aS)-10b demonstrated efficacy at restoring levator ani muscle mass to that of intact controls and exhibited > 50-fold selectivity for muscle over prostate.
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