Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity.

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Long YO, Higuchi RI, Caferro TR, Lau TL, Wu M, Cummings ML, Martinborough EA, Marschke KB, Chang WY, Lopez FJ, Karanewsky DS, Zhi L

Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity.

Bioorg Med Chem Lett. 2008 May 1;18(9):2967-71. doi: 10.1016/j.bmcl.2008.03.062. Epub 2008 Mar 23.

PubMed ID

18400499 [ View in PubMed

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Abstract

Modification on a lead series of [1,4]oxazino[3,2-g]quinolin-7-ones at the 2-position led to selective androgen receptor modulators with improved in vivo activity. The most potent analog (-)-33a exhibited full maintenance of levator ani muscle at 3mg/kg and reduced activity on ventral prostate weight in a 2-week orally-dosed and orchidectomized rat maintenance assay.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Bicalutamide	Androgen receptor	IC 50 (nM)	162	N/A	N/A	Details
Bicalutamide	Androgen receptor	Ki (nM)	151	N/A	N/A	Details
Stanolone	Androgen receptor	EC 50 (nM)	5.7	N/A	N/A	Details
Stanolone	Androgen receptor	Ki (nM)	0.9	N/A	N/A	Details