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Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones
- Source :
- Bioorganic & Medicinal Chemistry Letters. 17:5442-5446
- Publication Year :
- 2007
- Publisher :
- Elsevier BV, 2007.
-
Abstract
- A series of androgen receptor modulators based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones was synthesized and evaluated in an androgen receptor transcriptional activation assay. The most potent analogues from the series exhibited single-digit nanomolar potency in vitro. Compound 18h demonstrated full efficacy in the maintenance of muscle weight, at 10 mg/kg, with reduced activity in prostate weight in an in vivo model of androgen action.
- Subjects :
- Male
Models, Molecular
medicine.medical_specialty
medicine.drug_class
Clinical Biochemistry
Pharmaceutical Science
Quinolones
Biochemistry
Article
Cell Line
Structure-Activity Relationship
In vivo
Internal medicine
Oxazines
Drug Discovery
medicine
Animals
Humans
Potency
Structure–activity relationship
Testosterone
Receptor
Molecular Biology
Dose-Response Relationship, Drug
Chemistry
Organic Chemistry
Receptors, Somatotropin
Androgen
Rats
Androgen receptor
Endocrinology
Selective androgen receptor modulator
Receptors, Androgen
Molecular Medicine
Indicators and Reagents
Receptors, Progesterone
Orchiectomy
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 17
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....fb24be52ff66235cfadff901d5d77fd6