title: New 11 beta-aryl-substituted steroids exhibit both progestational and antiprogestational activity.
abstract: 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.
authors.affiliation: Department of Organic Chemistry, Southwest Foundation for Biomedical Research, San Antonio, Texas 78245-0549, USA.
authors.forename: P N
authors.initials: PN
authors.lastname: Rao
authors.forename: Z
authors.initials: Z
authors.lastname: Wang
authors.forename: J W
authors.initials: JW
authors.lastname: Cessac
authors.forename: R S
authors.initials: RS
authors.lastname: Rosenberg
authors.forename: D J
authors.initials: DJ
authors.lastname: Jenkins
authors.forename: E P
authors.initials: EP
authors.lastname: Diamandis
mesh_terms: 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
chemical_list: D009649:Norpregnadienes; D011372:Progestins