Bioorganic and Medicinal Chemistry Letters p. 5442 - 5446 (2007)
Update date:2022-08-04
Topics:
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
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.
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