Abstract
The SAR of C5' functional groups with terminal basic amines at the C6 aniline of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines is reported. Examples demonstrate potent inhibition of IGF-1R with 1000-fold selectivity over JNK1 and 3 in enzymatic assays.
MeSH terms
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MAP Kinase Kinase 4 / antagonists & inhibitors*
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Models, Molecular
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Protein Kinase Inhibitors / pharmacology*
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Pyrimidines / chemistry
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Pyrimidines / pharmacology*
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Pyrroles / chemistry
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Pyrroles / pharmacology*
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Receptor, IGF Type 1 / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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4,6-bis-anilino-1H-pyrrolo(2,3-d)pyrimidine
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Protein Kinase Inhibitors
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Pyrimidines
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Pyrroles
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Receptor, IGF Type 1
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MAP Kinase Kinase 4