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

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Higuchi RI, Thompson AW, Chen JH, Caferro TR, Cummings ML, Deckhut CP, Adams ME, Tegley CM, Edwards JP, Lopez FJ, Kallel EA, Karanewsky DS, Schrader WT, Marschke KB, Zhi L

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

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

PubMed ID
17703938 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
StanoloneAndrogen receptorIC 50 (nM)>10000N/AN/ADetails
StanoloneAndrogen receptorEC 50 (nM)5.7N/AN/ADetails