3-Amido-4-anilinocinnolines as a novel class of CSF-1R inhibitor

3-Amido-4-anilinocinnolines have been identified as potent and highly selective inhibitors of CSF-1R. The synthesis and SAR of these compounds is reported, along with some physical property, pharmacokinetic and kinase selectivity data.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-03, Vol.21 (5), p.1382-1384
Hauptverfasser:	Scott, David A., Dakin, Les A., Del Valle, David J., Bruce Diebold, R., Drew, Lisa, Gero, Thomas W., Ogoe, Claude A., Omer, Charles A., Repik, Galina, Thakur, Kumar, Ye, Qing, Zheng, Xiaolan
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemical synthesis Amides - chemistry Analytical, structural and metabolic biochemistry Aniline Compounds - chemical synthesis Aniline Compounds - chemistry Animals antagonists Biological and medical sciences Cinnoline CSF-1R Dogs Enzymes and enzyme inhibitors Fundamental and applied biological sciences. Psychology heterocyclic compounds Heterocyclic Compounds, 2-Ring - chemical synthesis Heterocyclic Compounds, 2-Ring - chemistry Kinase inhibitor macrophage colony-stimulating factor Medical sciences Mice Miscellaneous Molecular Structure pharmacokinetics Pharmacology. Drug treatments Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Rats receptor protein-tyrosine kinase Receptor, Macrophage Colony-Stimulating Factor - antagonists & inhibitors Structure-Activity Relationship structure-activity relationships synthesis Transferases
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Beschreibung
Zusammenfassung:	3-Amido-4-anilinocinnolines have been identified as potent and highly selective inhibitors of CSF-1R. The synthesis and SAR of these compounds is reported, along with some physical property, pharmacokinetic and kinase selectivity data.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.01.033