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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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2739385 | PMC |
| http://dx.doi.org/10.1016/j.bmcl.2007.07.034 | DOI Listing |
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