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 benzothiophene-based equilenin analogues.
Lugar
Charles W
CW
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA.
Magee
David
D
Adrian
Mary D
MD
Shetler
Pamela
P
Bryant
Henry U
HU
Dodge
Jeffrey A
JA
D000818:Animals; D004857:Equilin / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045166:Estradiol Congeners / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D005260:Female; D008958:Models, Molecular; D008968:Molecular Conformation; D009929:Organ Size / Q000187:drug effects; D010052:Ovariectomy; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014599:Uterus / Q000033:anatomy & histology / Q000187:drug effects
D045166:Estradiol Congeners; D004857:Equilin; C014482:dihydroequilin