Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 47, Issue 26, Pages 6435-6438Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm049194+
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Pathway-selective ligands for the estrogen receptor (ER) inhibit NF-kappaB-mediated inflammatory gene expression causing a reduction of cytokines, chemokines, adhesion molecules, and inflammatory enzymes. SAR development of a series of 4-(indazol-3-yl)phenols has led to the identification of WAY-169916 an orally active nonsteroidal ligand with the potential use in the treatment of rheumatoid arthritis without the classical proliferative effects associated with estrogens.
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