New 11 beta-aryl-substituted steroids exhibit both progestational and antiprogestational activity

• Published in: Steroids Vol. 63; no. 10; pp. 523 - 530
• Main Authors: Rao, PN, Wang, ZQ, Cessac, JW, Rosenberg, RS, Jenkins, DJA, Diamandis, EP
• Format: Journal Article
• Language: English
• Published: NEW YORK Elsevier 01.10.1998; Elsevier Science
• Subjects: Biochemistry & Molecular Biology; Biological and medical sciences; Endocrinology & Metabolism; Female; Hormones. Endocrine system; Humans; Life Sciences & Biomedicine; Magnetic Resonance Spectroscopy; Mass Spectrometry; Medical sciences; Molecular Structure; Norpregnadienes - pharmacology; Pharmacology. Drug treatments; Progestins - antagonists & inhibitors; Progestins - chemistry; Progestins - pharmacology; Science & Technology; Tumor Cells, Cultured; synthesis; antiprogestin; progestin; ANALOGS; AGONIST ACTIVITY; MIFEPRISTONE; CANCER; steroids; PSA gene regulation; steroid hormone receptors; CDB-2914; prostate-specific antigen; ANTIPROGESTERONE; Steroid; Agonist; Malignant tumor; In vitro; Ovarian hormone; Biological activity; Prostate specific antigen; Mammary gland diseases; Cell line; Antagonist; Mammary gland; Progesterone; Sex steroid hormone; Chemical synthesis; Hormonal receptor
• ISSN: 0039-128X; 1878-5867
• DOI: 10.1016/S0039-128X(98)00060-9

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. (Steroids 63:523-530, 1998) (C) 1998 by Elsevier Science Inc.