Abstract
A novel series of 2-amino-4-(7-azaindol-3-yl)pyrimidines was discovered as cyclin dependent kinase 1 (CDK1) inhibitors. The core structure was synthesized via Pd(II) catalyzed coupling reaction. A number of analogues showed good potency for CDK1 and exhibited cellular antiproliferation activity. The structure-activity relationship is described.
MeSH terms
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Amination
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Aza Compounds / chemical synthesis*
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Aza Compounds / chemistry
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Aza Compounds / pharmacology*
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CDC2 Protein Kinase / antagonists & inhibitors*
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CDC2 Protein Kinase / metabolism
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HeLa Cells
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Humans
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Inhibitory Concentration 50
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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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Pyrimidines / chemical synthesis
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Pyrimidines / chemistry*
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Pyrimidines / pharmacology*
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Structure-Activity Relationship
Substances
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Aza Compounds
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Protein Kinase Inhibitors
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Pyrimidines
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CDC2 Protein Kinase