New 11 beta-aryl-substituted steroids exhibit both progestational and antiprogestational activity.
The syntheses of three 11 beta-aryl-19-norpregna-4,9-dien-3-one derivatives with 17-spirolactone and 17 beta-hydroxy-17 alpha-cyanoethyl substitutions are described. The progesterone agonist/antagonist activities of the new compounds are investigated using a recently developed tissue culture system that relies on the progesterone agonist up-regulation of the prostate-specific antigen (PSA) gene in female breast tumor cell lines. Two of the newly synthesized compounds exhibit mixed agonistic/antagonistic progestational activity.
Rao
P N
PN
Department of Organic Chemistry, Southwest Foundation for Biomedical Research, San Antonio, Texas 78245-0549, USA.
Wang
Z
Z
Cessac
J W
JW
Rosenberg
R S
RS
Jenkins
D J
DJ
Diamandis
E P
EP
D005260:Female; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D015394:Molecular Structure; D009649:Norpregnadienes / Q000494:pharmacology*; D011372:Progestins / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
D009649:Norpregnadienes; D011372:Progestins