Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors.

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Moree WJ, Goldman P, Demaggio AJ, Christenson E, Herendeen D, Eksterowicz J, Kesicki EA, McElligott DL, Beaton G

Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5126-9. doi: 10.1016/j.bmcl.2008.07.091. Epub 2008 Jul 27.

PubMed ID

18713665 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
3,4-Dihydro-5-Methyl-Isoquinolinone	Poly [ADP-ribose] polymerase 1	IC 50 (nM)	160	8	23	Details