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

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Mitchell HJ, Dankulich WP, Hartman GD, Prueksaritanont T, Schmidt A, Vogel RL, Bai C, McElwee-Witmer S, Zhang HZ, Chen F, Leu CT, Kimmel DB, Ray WJ, Nantermet P, Gentile MA, Duggan ME, Meissner RS

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

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

PubMed ID

19606870 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Stanolone	Androgen receptor	IC 50 (nM)	1	N/A	N/A	Details
Stanolone	Androgen receptor	EC 50 (nM)	2	N/A	N/A	Details