| Literature DB >> 18289848 |
Mark J Wall1, 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, Mark R Player, Raymond J Patch, Carl L Manthey, Christopher Molloy, Bruce Tomczuk, Carl R Illig.
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 IC(50) 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.Entities:
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Year: 2008 PMID： 18289848 DOI： 10.1016/j.bmcl.2008.01.088
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823