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J Med Chem. 2009 Aug 13;52(15):4578-81. doi: 10.1021/jm900880r.

Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, P.O. Box 4, 770 Sumneytown Pike, West Point, Pennsylvania 19486, USA. Helen_mitchell2@merck.com

Abstract

A novel series of 16-substituted-4-azasteroids has been identified as potential tissue-selective androgen receptor modulators. These ligands display potent hAR binding and agonist activity, low virilizing potential, and good pharmacokinetic profiles in dogs. On the basis of its in vitro profile, 21 was evaluated in the OVX and ORX rat models and exhibited an osteoanabolic, tissue-selective profile.

PMID:
19606870
DOI:
10.1021/jm900880r
[Indexed for MEDLINE]

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