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.


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.

MeSH terms

  • Androgens
  • Animals
  • Azasteroids / chemical synthesis*
  • Azasteroids / pharmacology
  • Dogs
  • Drug Design
  • ERG1 Potassium Channel
  • Ether-A-Go-Go Potassium Channels / metabolism
  • Female
  • Humans
  • Male
  • Organ Specificity
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Androgen / drug effects*
  • Structure-Activity Relationship


  • AR protein, human
  • Androgens
  • Azasteroids
  • ERG1 Potassium Channel
  • Ether-A-Go-Go Potassium Channels
  • Receptors, Androgen