Abstract
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.
MeSH terms
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Administration, Oral
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Animals
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Humans
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Inhibitory Concentration 50
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Kinetics
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Models, Chemical
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Neoplasms / drug therapy*
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / chemistry
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Quinolines / chemistry*
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Quinolines / pharmacokinetics*
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Rats
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Receptor, Macrophage Colony-Stimulating Factor / antagonists & inhibitors*
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Receptor, Macrophage Colony-Stimulating Factor / chemistry*
Substances
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Antineoplastic Agents
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Protein Kinase Inhibitors
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Quinolines
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Receptor, Macrophage Colony-Stimulating Factor