17 alpha-Alkan (or alkyn) amide derivatives of estradiol as inhibitors of steroid-sulfatase activity

• Published in: Steroids Vol. 64; no. 12; pp. 825 - 833
• Main Authors: Boivin, RP, Labrie, F, Poirier, D
• Format: Journal Article
• Language: English
• Published: NEW YORK Elsevier 01.12.1999
• Subjects: Biochemistry & Molecular Biology; Endocrinology & Metabolism; Life Sciences & Biomedicine; Science & Technology; enzyme; cancel; 17-BETA-HYDROXYSTEROID DEHYDROGENASE; ESTRONE-SULFATASE; BREAST-CANCER-CELLS; CHEMICAL SYNTHESIS; steroid sulfatase; POTENT; ANTIESTROGENIC ACTIVITY; inhibitor; BIOLOGICAL-ACTIVITY; GROWTH; ENDOMETRIAL; alkylamide; AROMATASE INHIBITORS; steroid; estradiol

To develop inhibitors of steroid sulfatase without residual estrogenic activity, we have designed a series of estradiol (E-2) derivatives bearing an alkan (or alkyn) amide side chain at position 17 alpha. A hydrophobic alkyl group was selected from our previous study where 17 alpha-octyl-E-2 was fou...