Toward Selective ERβ Agonists for Central Nervous System Disorders: Synthesis and Characterization of Aryl Benzthiophenes
- 26 February 2002
- journal article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 45 (7) , 1399-1401
- https://doi.org/10.1021/jm015577l
Abstract
In an effort to identify selective ligands for the estrogen receptor subtype ERβ, a series of aryl benzthiophenes was synthesized. In a radioligand binding assay and reporter gene assays in HeLa and SH-SY5Y cells, compounds were characterized as ERβ-selective agonists. By targeting ERβ in the brain, these compounds could lead to drugs able to separate the beneficial effects of estrogens on mood, learning, and memory from side effects such as the stimulation of endometrial and breast cancer.Keywords
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