Title of article
Synthesis and evaluation of novel 3,4,6-substituted 2-quinolones as FMS kinase inhibitors
Author/Authors
Mark J. Wall، نويسنده , , Jinsheng Chen، نويسنده , , Sanath Meegalla، نويسنده , , Shelley K. Ballentine، نويسنده , , Kenneth J. Wilson، نويسنده , , Renee L. DesJarlais، نويسنده , , Paul B. Sigler and Carsten Schubert، نويسنده , , Margery A. Chaikin، نويسنده , , Carl Crysler، نويسنده , , Ioanna P. Petrounia، نويسنده , , Robert R. Donatelli، نويسنده , , Edward J. Yurkow، نويسنده , , Lisa Boczon، نويسنده , , Marie Mazzulla، نويسنده , , Mark R. Player، نويسنده , , Raymond J. Patch، نويسنده , , Carl L. Manthey، نويسنده , , Christopher Molloy، نويسنده , , Bruce Tomczuk، نويسنده , , Carl R. Illig، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
6
From page
2097
To page
2102
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.
Keywords
M-CSF , FMS , cFMS , Colony-stimulating factor-1 receptor , CSF-1 , 2-Quinolones
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799306
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