Control of Chronic Inflammation with Pathway Selective Estrogen Receptor Ligands

Author(s): Robert J. Steffan, Edward Matelan, Mark A. Ashwell, William J. Moore, William R. Solvibile, Eugene Trybulski, Christopher C. Chadwick, Susan Chippari, Thomas Kenney, Richard C. Winneker, Amy Eckert, Lisa Borges-Marcucci, Steven J. Adelman, Zhang Xu, Lydia Mosyak, Douglas C. Harnish

Journal Name: Current Topics in Medicinal Chemistry

Volume 6 , Issue 2 , 2006

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The discovery of novel intervention points in the inflammatory pathway has been a focus of drug development in recent years. We have identified pathway selective ligands for the estrogen receptor (ER) that inhibit NF-kB 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 non-steroidal ligand with the potential use in the treatment of inflammatory diseases without the classical proliferative effects associated with non-selective estrogens.

Keywords: Estrogen receptor, ER, nuclear factor kappa B, NF-kB

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Article Details

Year: 2006
Page: [103 - 111]
Pages: 9
DOI: 10.2174/156802606775270279
Price: $65

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