Identification of 3-amido-4-anilinoquinolines as potent and selective inhibitors of CSF-1R kinase

3-Amido-4-anilinoquinolines are potent and highly selective inhibitors of CSF-1R. Their synthesis and SAR is reported, along with initial efforts to optimize the physical properties and PK through modifications at the quinoline 6- and 7-positions.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-02, Vol.19 (3), p.697-700
Hauptverfasser:	Scott, David A., Balliet, Carrie L., Cook, Donald J., Davies, Audrey M., Gero, Thomas W., Omer, Charles A., Poondru, Srinivasu, Theoclitou, Maria-Elena, Tyurin, Boris, Zinda, Michael J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Biological and medical sciences Chemistry, Pharmaceutical - methods CSF-1R Drug Design General aspects Humans Inhibitory Concentration 50 Kinase inhibitor Kinetics Medical sciences Models, Chemical Neoplasms - drug therapy Pharmacology. Drug treatments Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Quinoline Quinolines - chemistry Quinolines - pharmacokinetics Rats Receptor, Macrophage Colony-Stimulating Factor - antagonists & inhibitors Receptor, Macrophage Colony-Stimulating Factor - chemistry
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Beschreibung
Zusammenfassung:	3-Amido-4-anilinoquinolines are potent and highly selective inhibitors of CSF-1R. Their synthesis and SAR is reported, along with initial efforts to optimize the physical properties and PK through modifications at the quinoline 6- and 7-positions.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2008.12.046