2-Phenylspiroindenes: a novel class of selective estrogen receptor modulators (SERMs)

• Published in: Bioorganic & medicinal chemistry letters Vol. 13; no. 3; pp. 479 - 483
• Main Authors: Blizzard, Timothy A, Morgan, II, Jerry D, Mosley, Ralph T, Birzin, Elizabeth T, Frisch, Katalin, Rohrer, Susan P, Hammond, Milton L
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 10.02.2003; Elsevier
• Subjects: Alkylation; Animals; Biological and medical sciences; Borohydrides; Crystallography, X-Ray; Hormones. Endocrine system; Humans; In Vitro Techniques; Indenes - chemical synthesis; Indenes - pharmacology; Indicators and Reagents; Medical sciences; Pharmacology. Drug treatments; Raloxifene Hydrochloride - pharmacology; Rats; Receptors, Estrogen - drug effects; Selective Estrogen Receptor Modulators - chemical synthesis; Selective Estrogen Receptor Modulators - pharmacology; Spiro Compounds - chemical synthesis; Spiro Compounds - pharmacology; Structure-Activity Relationship; Estrogen receptor; Rat; Nitrogen heterocycle; Selectivity; Structure activity relation; Piperidine derivatives; Aromatic compound; Indene derivatives; Chemical synthesis; Non steroid compound; Human; Modulator; Rodentia; Aminoether; Tetracyclic compound; In vitro; Spiran; Vertebrata; Biological fixation; Mammalia; Animal; Phenols; Affinity; Raloxifene; Hormonal receptor
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/S0960-894X(02)00985-X

A series of 2-phenylspiroindenes was prepared. The most active analogue ( 2) was found to be comparable in potency to raloxifene ( 1) as an estrogen receptor ligand. A series of 2-phenylspiroindenes was prepared. The most active analogue ( 2) was found to be comparable in potency to raloxifene as an estrogen receptor ligand.