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J Med Chem. 2006 Dec 28;49(26):7596-9.

Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold.

Author information

1
Bristol-Myers Squibb Pharmaceutical Research Institute, Post Office Box 5400, Princeton, NJ 08543-5400, USA. chongqing.sun@bms.com

Abstract

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.

PMID:
17181141
DOI:
10.1021/jm061101w
[Indexed for MEDLINE]

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