Abstract
Checkpoint kinase-1 (Chk1, CHEK1) is a Ser/Thr protein kinase that mediates the cellular response to DNA-damage. A novel class of 2-ureido thiophene carboxamide urea (TCU) Chk1 inhibitors is described. Inhibitors in this chemotype were optimized for cellular potency and selectivity over Cdk1.
MeSH terms
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Amides / chemistry
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Apoptosis
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Carbon / chemistry
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Cell Cycle
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Checkpoint Kinase 1
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Chemistry, Pharmaceutical / methods*
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DNA Damage
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Drug Design
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Humans
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Inhibitory Concentration 50
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Models, Chemical
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Phenyl Ethers / chemistry
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Protein Kinase Inhibitors / chemical synthesis*
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Protein Kinase Inhibitors / pharmacology*
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Protein Kinases / chemistry*
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Thiophenes / chemistry
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Urea / chemistry
Substances
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Amides
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Phenyl Ethers
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Protein Kinase Inhibitors
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Thiophenes
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Carbon
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Urea
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Protein Kinases
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CHEK1 protein, human
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Checkpoint Kinase 1