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3-amido-4-anilinoquinolines as CSF-1R kinase inhibitors 2: Optimization of the PK profile.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Feb 01; Vol. 19 (3), pp. 701-5. Date of Electronic Publication: 2008 Dec 14. - Publication Year :
- 2009
-
Abstract
- The optimization of compounds from the 3-amido-4-anilinoquinolines series of CSF-1R kinase inhibitors is described. The series has excellent activity and kinase selectivity. Excellent physical properties and rodent PK profiles were achieved through the introduction of cyclic amines at the quinoline 6-position. Compounds with good activity in a mouse PD model measuring inhibition of pCSF-1R were identified.
- Subjects :
- Amines chemistry
Animals
Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
ERG1 Potassium Channel
Ether-A-Go-Go Potassium Channels metabolism
Humans
Inhibitory Concentration 50
Kinetics
Mice
Models, Chemical
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors chemistry
Rats
Chemistry, Pharmaceutical methods
Neoplasms drug therapy
Quinolines chemistry
Quinolines pharmacokinetics
Receptor, Macrophage Colony-Stimulating Factor antagonists & inhibitors
Receptor, Macrophage Colony-Stimulating Factor chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 19
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 19114305
- Full Text :
- https://doi.org/10.1016/j.bmcl.2008.12.044