Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 7, Pages 1399-1401Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm015577l
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In an effort to identify selective ligands for the estrogen receptor subtype ERbeta, 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 ERbeta-selective agonists. By targeting ER 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.
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