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

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 weigh...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-05, Vol.18 (9), p.2967-2971
Hauptverfasser:	LONG, Yun Oliver, HIGUCHI, Robert I, KARANEWSKY, Donald S, LIN ZHI, CAFERRO, Thomas R, LAU, Thomas L. S, MIN WU, CUMMINGS, Marquis L, MARTINBOROUGH, Esther A, MARSCHKE, Keith B, CHANG, William Y, LOPEZ, Francisco J
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Anabolic Agents - chemical synthesis Anabolic Agents - pharmacology Androgen Receptor Antagonists Androgens Animals Biological and medical sciences Hormones. Endocrine system Male Medical sciences Models, Chemical Orchiectomy Organ Size - drug effects Oxazines - chemical synthesis Oxazines - pharmacology Pharmacology. Drug treatments Prostate - anatomy & histology Prostate - drug effects Quinolones - chemical synthesis Quinolones - pharmacology Rats Rats, Sprague-Dawley Receptors, Androgen Structure-Activity Relationship Testosterone - pharmacology
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Zusammenfassung:	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.
ISSN:	0960-894X 0968-0896 1464-3405 1464-3391
DOI:	10.1016/j.bmcl.2008.03.062