Abstract
A remarkably concise, chromatography-free route to the parent compound of the paullone family of cyclin-dependent kinase (CDK) inhibitors is reported. A similar strategy allowed the synthesis of the hitherto missing 9-azapaullone and its protonated, N-oxidised and N-alkylated derivatives. Screening studies identified an active and strongly selective inhibitor of CDK9/cyclin T.
2010 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Aza Compounds / chemistry*
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Benzazepines / chemical synthesis
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Benzazepines / chemistry*
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Benzazepines / pharmacology
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Cyclin T / antagonists & inhibitors
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Cyclin T / metabolism
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Cyclin-Dependent Kinases / antagonists & inhibitors*
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Cyclin-Dependent Kinases / metabolism
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Glycogen Synthase Kinase 3 / antagonists & inhibitors*
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Glycogen Synthase Kinase 3 / metabolism
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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
Substances
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Aza Compounds
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Benzazepines
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Cyclin T
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Protein Kinase Inhibitors
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paullone
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Cyclin-Dependent Kinases
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Glycogen Synthase Kinase 3