Abstract
CHK-1 is one of the key enzymes regulating checkpoints in cellular growth cycles. Novel 4-(amino-alkylamino)-3-benzimidazole-quinolinones were prepared and assayed for their ability to inhibit CHK-1. These compounds are potent cell permeable CHK-1 inhibitors and showed synergistic effect with a DNA-damaging agent, camptothecin.
MeSH terms
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Alkylation
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Amination
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Benzimidazoles / chemistry*
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Cell Line, Tumor
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Checkpoint Kinase 1
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Crystallography, X-Ray
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Humans
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Inhibitory Concentration 50
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Models, Molecular
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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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Protein Kinases / chemistry
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Protein Kinases / metabolism*
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Quinolones / chemical synthesis
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Quinolones / chemistry*
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Quinolones / pharmacology*
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Structure-Activity Relationship
Substances
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Benzimidazoles
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Protein Kinase Inhibitors
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Quinolones
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benzimidazole
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Protein Kinases
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Checkpoint Kinase 1