| Autor: |
Higuchi RI; Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA. rhiguchi@ligand.com, Thompson AW, Chen JH, Caferro TR, Cummings ML, Deckhut CP, Adams ME, Tegley CM, Edwards JP, López FJ, Kallel EA, Karanewsky DS, Schrader WT, Marschke KB, Zhi L |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Oct 01; Vol. 17 (19), pp. 5442-6. Date of Electronic Publication: 2007 Jul 25. |
| DOI: |
10.1016/j.bmcl.2007.07.034 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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