Back to Search
Start Over
Design, Synthesis, and Biological Evaluation of 16-Substituted 4-Azasteroids as Tissue-Selective Androgen Receptor Modulators (SARMs)
- Source :
- Journal of Medicinal Chemistry. 52:4578-4581
- Publication Year :
- 2009
- Publisher :
- American Chemical Society (ACS), 2009.
-
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.
- Subjects :
- Male
Azasteroids
Agonist
ERG1 Potassium Channel
medicine.medical_specialty
medicine.drug_class
medicine.medical_treatment
Steroid
Rats, Sprague-Dawley
Structure-Activity Relationship
Dogs
Internal medicine
Drug Discovery
medicine
Animals
Humans
music
music.instrument
Chemistry
Biological activity
Ether-A-Go-Go Potassium Channels
In vitro
Azasteroid
Rats
Androgen receptor
Endocrinology
Selective androgen receptor modulator
Organ Specificity
Receptors, Androgen
Drug Design
Androgens
Molecular Medicine
Female
Subjects
Details
- ISSN :
- 15204804 and 00222623
- Volume :
- 52
- Database :
- OpenAIRE
- Journal :
- Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....5c999347b3114925de3ef07c508765a6