Inflammation is recognized as a key component of diseases such as atherosclerosis, rheumatoid arthritis, and inflammatory bowel disease. It has been reported that pathway-selective, estrogen-receptor (ER) ligands capable of indirectly inhibiting NF-KB-mediated inflammatory gene expression result in a reduction of cytokines, chemokines, adhesion molecules, and inflammatory enzymes. These ligands lacking conventional estrogenic activity, such as the stimulation of uterine cell proliferation, would be of potential use in the treatment of chronic inflammatory diseases. A series of 3-(3-hydroxybenzoyl)indazoles were identified as pathway-selective ER ligands capable of indirectly inhibiting NF-KB gene transcription. Their synthesis and activity are described.