Abstract
A novel series of quinolinyl-methylene-thiazolinones has been identified as potent and selective cyclin-dependent kinase 1 (CDK1) inhibitors. Their synthesis and structure activity relationships (SAR) are described. Representative compounds from this class reversibly inhibit CDK1 activity in vitro, and block cell cycle progression in human tumor cell lines, suggesting a potential use as antitumor agents.
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / pharmacology
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CDC2 Protein Kinase / antagonists & inhibitors*
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Cell Line, Tumor
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Drug Screening Assays, Antitumor
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Humans
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / pharmacology
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Structure-Activity Relationship
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Thiazoles / chemical synthesis*
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Thiazoles / pharmacology
Substances
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Antineoplastic Agents
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Protein Kinase Inhibitors
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Thiazoles
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CDC2 Protein Kinase