Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376238 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
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.
Graphical abstractPotent PARP-1 inhibitors were identified in a tricyclic pyrazolo pyridine-2-one series with nanomolar binding affinity and submicromar activity in a cell-based chemosensitization assay.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Wilna J. Moree, Phyllis Goldman, Anthony J. Demaggio, Erik Christenson, Dan Herendeen, John Eksterowicz, Edward A. Kesicki, David L. McElligott, Graham Beaton,