Abstract
Chk1 inhibitors have emerged as a novel class of neoplastic agents for abrogating the G2 DNA damage checkpoint arrest. Analogs of the Chk1 inhibitor, 3-ethylidene-1,3-dihydro-indol-2-one, were synthesized and tested in vitro for their inhibitory activities. The most promising compound identified from this series is analog 28, which possesses potent enzymatic and cellular activities.
MeSH terms
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Cell Proliferation / drug effects
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Checkpoint Kinase 1
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Crystallography, X-Ray
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Drug Design
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Drug Evaluation, Preclinical
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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HeLa Cells
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Humans
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Models, Molecular
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Molecular Structure
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Protein Kinases / drug effects*
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Structure-Activity Relationship
Substances
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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