Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376842 | Bioorganic & Medicinal Chemistry Letters | 2008 | 6 Pages |
Abstract
A series of 3,4,6-substituted 2-quinolones has been synthesized and evaluated as inhibitors of the kinase domain of macrophage colony-stimulating factor-1 receptor (FMS). The fully optimized compound, 4-(4-ethyl-phenyl)-3-(2-methyl-3H-imidazol-4-yl)-2-quinolone-6-carbonitrile 21b, has an IC50 of 2.5 nM in an in vitro assay and 5.0 nM in a bone marrow-derived macrophage cellular assay. Inhibition of FMS signaling in vivo was also demonstrated in a mouse pharmacodynamic model.
Graphical abstractA series of 3,4,6-substituted 2-quinolones has been synthesized and evaluated as FMS inhibitors.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
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Authors
Mark J. Wall, Jinsheng Chen, Sanath Meegalla, Shelley K. Ballentine, Kenneth J. Wilson, Renee L. DesJarlais, Carsten Schubert, Margery A. Chaikin, Carl Crysler, Ioanna P. Petrounia, Robert R. Donatelli, Edward J. Yurkow, Lisa Boczon, Marie Mazzulla,