1. Tetrahydroisoquinolines as subtype selective estrogen agonists/antagonists.
- Author
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Chesworth R, Zawistoski MP, Lefker BA, Cameron KO, Day RF, Mangano FM, Rosati RL, Colella S, Petersen DN, Brault A, Lu B, Pan LC, Perry P, Ng O, Castleberry TA, Owen TA, Brown TA, Thompson DD, and DaSilva-Jardine P
- Subjects
- Cell Line, Tumor, Cell Proliferation drug effects, Estrogen Receptor alpha chemistry, Estrogen Receptor beta chemistry, Female, Humans, Inhibitory Concentration 50, Ligands, Protein Binding, Selective Estrogen Receptor Modulators pharmacology, Structure-Activity Relationship, Tetrahydroisoquinolines chemical synthesis, Selective Estrogen Receptor Modulators chemical synthesis, Tetrahydroisoquinolines pharmacology
- Abstract
Two series of 6-hydroxy and 7-hydroxy tetrahydroisoquinolines were prepared. Evaluating a range of C-1, C-4, and N-substituents led to the discovery of ER alpha and ER beta selective analogs.
- Published
- 2004
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