Identification and SAR of novel pyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1)

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 3, 2010, Pages 1094-1099

  Pescatore, Giovanna ^a   Branca, Danila ^a   Fiore, Fabrizio ^a   Kinzel, Olaf ^a   Bufi, Laura Llauger ^a   Muraglia, Ester ^a   Orvieto, Federica ^a   Rowley, Michael ^a   Toniatti, Carlo ^a   Torrisi, Caterina ^a   Jones, Philip ^a  

^a IRBM   (Italy)

Author keywords

BRCA1; Oncology; PARP 1; Poly(ADP ribose) polymerase; Pyrrolo 1,2 a pyrazin 1(2H) one; Selectivity

Indexed keywords

2 (2 METHYL 2 PYRROLIDINYL) 1H BENZIMIDAZOLE 4 CARBOXAMIDE; 8 FLUORO 3,4 DIHYDRO 2 [4 (METHYLAMINOMETHYL)PHENYL]PYRROLO[3,4,5 E,F][2]BENZAZEPIN 6(5H) ONE; AGO 14699; ANTINEOPLASTIC AGENT; BRCA1 PROTEIN; MK 4827; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE 1; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE INHIBITOR; OLAPARIB; PYRAZINE DERIVATIVE; UNCLASSIFIED DRUG; BRCA1 PROTEIN, HUMAN; INDOLIZINE; INDOLIZINE DERIVATIVE; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE; PARP1 PROTEIN, HUMAN; PROTEIN BINDING;

ANIMAL EXPERIMENT; ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER CELL; CELL PROLIFERATION; DRUG CLEARANCE; DRUG IDENTIFICATION; DRUG STRUCTURE; HUMAN; HUMAN CELL; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMISTRY; COMPARATIVE STUDY; DEFICIENCY; DRUG EFFECTS; ENZYMOLOGY; HELA CELL LINE; LIVER MICROSOME; METABOLISM; PHYSIOLOGY; TUMOR CELL LINE; X RAY CRYSTALLOGRAPHY;

ANIMALS; BRCA1 PROTEIN; CELL LINE, TUMOR; CRYSTALLOGRAPHY, X-RAY; HELA CELLS; HUMANS; INDOLIZINES; MICROSOMES, LIVER; POLY(ADP-RIBOSE) POLYMERASES; PROTEIN BINDING; PYRAZINES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 74349126956     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.12.026     Document Type: Article

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