[Heterocyclic annulated steroids from 2-hydroxymethylene-canrenone].
A-ring annulated heterocycles, the isoxazole 6, the pyrazoles 8 and the pyrimidines 9 are prepared starting from 2-hydroxymethylene canrenone 1. Binding studies were carried out with the compounds 1 and 6-8 using estrogen, progesterone, androgen, gluco- and mineralocorticoid receptors as well as the serum proteins SHBG and CBG: the substances were inactive on the receptor level. 1, 7 and 8a show weak binding affinity to CBG.
Görlitzer
K
K
Institut für Pharmazeutische Chemie, Technischen Universität Braunschweig.
Moormann
P
P
Pollow
K
K
Schaffrath
M
M
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001798:Blood Proteins / Q000378:metabolism; D002192:Canrenone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D051381:Rats; D017208:Rats, Wistar; D011956:Receptors, Cell Surface / Q000378:metabolism*
C093222:2-methylenecanrenone; D001798:Blood Proteins; D011956:Receptors, Cell Surface; D002192:Canrenone
Heterocyclisch anellierte Steroide aus 2-Hydroxymethylen-canrenon.