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Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors |
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| Authors: | Moree Wilna J Goldman Phyllis Demaggio Anthony J Christenson Erik Herendeen Dan Eksterowicz John Kesicki Edward A McElligott David L Beaton Graham |
| Institution: | Deltagen Research Laboratories (Former CombiChem, Inc.), 4570 Executive Drive, Suite 400, San Diego, CA 92121, USA. wmoree@neurocrine.com |
| 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. |
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