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Bioorg Med Chem Lett. 2007 Oct 1;17(19):5442-6. Epub 2007 Jul 25.

Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones.

Author information

1
Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA. rhiguchi@ligand.com

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.

PMID:
17703938
PMCID:
PMC2739385
DOI:
10.1016/j.bmcl.2007.07.034
[Indexed for MEDLINE]
Free PMC Article

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