Abstract
A pyrimidin-4-yl-urea motif forming a pseudo ring by intramolecular hydrogen bonding has been designed to mimic the pyrido[2,3-d]pyrimidin-7-one core structure of a well-established class of protein kinase inhibitors. Potent inhibition of a number of protein kinases was obtained with the first prototype compound synthesized to probe the design concept.
MeSH terms
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Amino Acids / chemistry
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Amino Acids / pharmacology
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Drug Design*
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Models, Molecular*
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Molecular Conformation
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Molecular Mimicry
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Molecular Structure
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Protein Kinase Inhibitors / chemical synthesis*
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Protein Kinase Inhibitors / chemistry
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Protein Kinase Inhibitors / pharmacology*
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Pyridones / chemistry*
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Pyridones / pharmacology*
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Pyrimidines / chemical synthesis*
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Pyrimidines / chemistry
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Pyrimidines / pharmacology*
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Structure-Activity Relationship
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Urea / analogs & derivatives*
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Urea / chemical synthesis*
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Urea / chemistry
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Urea / pharmacology*
Substances
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Amino Acids
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PD 166285
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Protein Kinase Inhibitors
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Pyridones
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Pyrimidines
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Urea