B-ring unsaturated estrogens: biological evaluation of 17alpha-Dihydroequilein and novel B-Nor-6-thiaequilenins as tissue selective estrogens

The pharmacology and SAR of representative equine estogens is described. 17alpha-Dihydroequilenin was found to prevent bone loss after 5 weeks of oral administration to ovariectomized rats. The stereochemical significance of the D-ring and the C/D ring juncture was investigated with a series of benz...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-12, Vol.13 (24), p.4281-4284
Hauptverfasser:	Lugar, 3rd, Charles W, Magee, David, Adrian, Mary D, Shetler, Pamela, Bryant, Henry U, Dodge, Jeffrey A
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Equilin - analogs & derivatives Equilin - chemical synthesis Equilin - chemistry Equilin - pharmacology Estradiol Congeners - administration & dosage Estradiol Congeners - chemical synthesis Estradiol Congeners - chemistry Estradiol Congeners - pharmacology Female Models, Molecular Molecular Conformation Organ Size - drug effects Ovariectomy Rats Stereoisomerism Structure-Activity Relationship Uterus - anatomy & histology Uterus - drug effects
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Zusammenfassung:	The pharmacology and SAR of representative equine estogens is described. 17alpha-Dihydroequilenin was found to prevent bone loss after 5 weeks of oral administration to ovariectomized rats. The stereochemical significance of the D-ring and the C/D ring juncture was investigated with a series of benzothiophene-based equilenin analogues.
ISSN:	0960-894X