title: Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors.
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.
authors: Deltagen Research Laboratories (Former CombiChem, Inc.), 4570 Executive Drive, Suite 400, San Diego, CA 92121, USA. wmoree@neurocrine.com
authors: Wilna J
authors: WJ
authors: Moree
authors: Phyllis
authors: P
authors: Goldman
authors: Anthony J
authors: AJ
authors: Demaggio
authors: Erik
authors: E
authors: Christenson
authors: Dan
authors: D
authors: Herendeen
authors: John
authors: J
authors: Eksterowicz
authors: Edward A
authors: EA
authors: Kesicki
authors: David L
authors: DL
authors: McElligott
authors: Graham
authors: G
authors: Beaton
mesh_terms: D000818:Animals; D002645:Chickens; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D000067856:Poly(ADP-ribose) Polymerase Inhibitors; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011728:Pyridones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D000067856:Poly(ADP-ribose) Polymerase Inhibitors; D011720:Pyrazoles; D011728:Pyridones