Abstract
The synthesis and structure-activity relationships (SAR) of Chk1 inhibitors based on a 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one core are described. Specifically, an exploration of the 7 and 8 positions on this previously disclosed core afforded compounds with improved enzymatic and cellular potency.
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / pharmacology*
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Benzodiazepinones / chemical synthesis
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Benzodiazepinones / pharmacology*
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Cell Line, Tumor / drug effects
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Checkpoint Kinase 1
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Drug Design*
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacology*
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HeLa Cells
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Humans
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Models, Chemical
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Protein Binding
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Protein Kinases / metabolism*
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Benzodiazepinones
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Enzyme Inhibitors
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Protein Kinases
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CHEK1 protein, human
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Checkpoint Kinase 1