1.
Bioorg Med Chem Lett
; 18(9): 2967-71, 2008 May 01.
Article
in English
| MEDLINE
| ID: mdl-18400499
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.
Subject(s)
Anabolic Agents/pharmacology , Oxazines/pharmacology , Prostate/drug effects , Quinolones/pharmacology , Receptors, Androgen , Administration, Oral , Anabolic Agents/chemical synthesis , Androgen Receptor Antagonists , Androgens , Animals , Male , Models, Chemical , Orchiectomy , Organ Size/drug effects , Oxazines/chemical synthesis , Prostate/anatomy & histology , Quinolones/chemical synthesis , Rats , Rats, Sprague-Dawley , Structure-Activity Relationship , Testosterone/pharmacology
2.
Bioorg Med Chem Lett
; 17(15): 4158-62, 2007 Aug 01.
Article
in English
| MEDLINE
| ID: mdl-17553679
ABSTRACT
A series of 5-benzylidene-1,2-dihydro-2,2,4-trimethyl-5H-1-aza-6-oxa-chrysenes was synthesized and profiled for their ability to act as selective glucocorticoid receptor modulators (SGRMs). The synthesis and structure-activity relationships for this series of compounds are presented.
