454170-05-9Relevant articles and documents
Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones
Higuchi, Robert I.,Thompson, Anthony W.,Chen, Jyun-Hung,Caferro, Thomas R.,Cummings, Marquis L.,Deckhut, Charlotte P.,Adams, Mark E.,Tegley, Christopher M.,Edwards, James P.,Lopez, Francisco J.,Kallel, E. Adam,Karanewsky, Donald S.,Schrader, William T.,Marschke, Keith B.,Zhi, Lin
, p. 5442 - 5446 (2007)
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.
