Abstract
The optimization of imidazo[1,2-a]pyridine inhibitors as potent and selective inhibitors of IGF-1R is presented. Further optimization of oral exposure in mice is also discussed. Detailed selectivity, in vitro activity, and in vivo PK profiles of an optimized compound is also highlighted.
MeSH terms
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Administration, Oral
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Aniline Compounds / chemistry
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Animals
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Cell Line, Tumor
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Chemistry, Pharmaceutical / methods*
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Crystallography, X-Ray
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Drug Design
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Humans
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Inhibitory Concentration 50
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Mice
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Models, Chemical
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Molecular Conformation
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Pyridines / chemical synthesis
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Pyridines / chemistry*
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Pyridines / pharmacology
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Receptor, IGF Type 1 / antagonists & inhibitors*
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Receptor, IGF Type 1 / chemistry*
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Receptor, Insulin / metabolism
Substances
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Aniline Compounds
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Pyridines
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Receptor, IGF Type 1
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Receptor, Insulin
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imidazo(1,2-a)pyridine
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aniline