Abstract
A novel class of PARP-1 inhibitors was identified containing a non-aromatic heterocycle or carbocycle fused to a pyrazolo pyridin-2-one. Compounds displayed low nanomolar binding activity in the PARP-1 binding assay and submicromolar activity in a cell based chemosensitization assay.
MeSH terms
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Animals
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Chickens
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Combinatorial Chemistry Techniques
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Drug Design
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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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Molecular Structure
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Poly(ADP-ribose) Polymerase Inhibitors*
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Pyrazoles* / chemical synthesis
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Pyrazoles* / chemistry
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Pyrazoles* / pharmacology
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Pyridones* / chemical synthesis
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Pyridones* / chemistry
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Pyridones* / pharmacology
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Poly(ADP-ribose) Polymerase Inhibitors
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Pyrazoles
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Pyridones