Abstract
A novel series of aminopyrimidine IKK2 inhibitors have been developed which show excellent in vitro inhibition of this enzyme and good selectivity over the IKK1 isoform. The relative potency and selectivity of these compounds has been rationalized using QSAR and structure-based modelling.
MeSH terms
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology
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I-kappa B Kinase
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Protein Serine-Threonine Kinases / antagonists & inhibitors*
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Protein Serine-Threonine Kinases / metabolism*
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Pyrimidines / chemical synthesis*
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Pyrimidines / pharmacology
Substances
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Enzyme Inhibitors
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Pyrimidines
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Protein Serine-Threonine Kinases
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I-kappa B Kinase