329229-75-6Relevant articles and documents
Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones
Higuchi, Robert I.,Arienti, Kristen L.,López, Francisco J.,Mani, Neelakhanda S.,Mais, Dale E.,Caferro, Thomas R.,Long, Yun Oliver,Jones, Todd K.,Edwards, James P.,Zhi, Lin,Schrader, William T.,Negro-Vilar, Andrés,Marschke, Keith B.
, p. 2486 - 2496 (2008/02/01)
Recent interest in orally available androgens has fueled the search for new androgens for use in hormone replacement therapy and as anabolic agents. In pursuit of this, we have discovered a series of novel androgen receptor modulators derived from 7H-[1,4]oxazino[3,2-g]quinolin-7-ones. These compounds were synthesized and evaluated in competitive binding assays and an androgen receptor transcriptional activation assay. A number of compounds from the series demonstrated single-digit nanomolar agonist activity in vitro. In addition, lead compound (R)-16e was orally active in established rodent models that measure androgenic and anabolic properties of these agents. In this assay, (R)-16e demonstrated full efficacy in muscle and only partially stimulated the prostate at 100 mg/kg. These data suggest that these compounds may be utilized as selective androgen receptor modulators or SARMs. This series represents a novel class of compounds for use in androgen replacement therapy.
Tricyclic quinolinone and tricyclic quinoline androgen receptor modulator compounds and methods
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, (2008/06/13)
Novel non-steroidal tricyclic quinolinone and tricyclic quinoline compounds and compositions that are agonists, partial agonists and/or antagonists for androgen receptors (AR), their preparation and their uses are described.
