way-169916 and Chronic-Disease

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-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 non-steroidal ligand with the potential use in the treatment of inflammatory diseases without the classical proliferative effects associated with non-selective estrogens.

Topics: Anti-Inflammatory Agents, Non-Steroidal; Chronic Disease; Humans; Inflammation; Ligands; Molecular Structure; Pyrazoles; Receptors, Estrogen; Structure-Activity Relationship