Discovery of Potent, Orally-active, and Muscle-selective Androgen Receptor Modulators Based on an N-aryl-hydroxybicyclohydantoin Scaffold.
From: Bristol-Myers Squibb Pharmaceutical Research Institute, Post Office Box 5400, Princeton, NJ 08543-5400, USA. chongqing.sun@bms.com
Journal of medicinal chemistry
- Publish Date: Dec 2006
- ISSN: 0022-2623
- Volume: 49
- Issue: 26
- Pages: 7596-9
- Medium: Print
- Language: English
- Citation (JAMA): Sun Chongqing, Robl Jeffrey A, Wang Tammy C, et al. Discovery of Potent, Orally-active, and Muscle-selective Androgen Receptor Modulators Based on an N-aryl-hydroxybicyclohydantoin Scaffold.. J. Med. Chem. Dec 2006;49:7596-9
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.
Mesh Headings (Keywords): Administration, Oral, Animals, Breast Neoplasms, Bridged Compounds, Cells, Cultured, Dihydrotestosterone, Humans, Hydantoins, Luciferases, Male, Mice, Muscle, Skeletal, Muscular Atrophy, Myoblasts, Rats, Receptors, Androgen, Trans-Activation (Genetics)
Check for Full Text / PubMed Unique Identifier (PMID): 17181141
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