Development of substituted 6-[4-fluoro-3-(piperazin-1-ylcarbonyl)benzyl]-4,5-dimethylpyridazin-3(2H)-ones as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors active in BRCA deficient cells

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 3, 2010, Pages 1100-1105

  Ferrigno, Federica ^a   Branca, Danila ^a   Kinzel, Olaf ^a   Lillini, Samuele ^a   Llauger Bufi, Laura ^a   Monteagudo, Edith ^a   Muraglia, Ester ^a   Rowley, Michael ^a   Schultz Fademrecht, Carsten ^a   Toniatti, Carlo ^a   Torrisi, Caterina ^a   Jones, Philip ^a  

^a IRBM   (Italy)

Author keywords

6 4 Fluoro 3 (piperazin 1 ylcarbonyl)benzyl 4,5 dimethylpyridazin 3(2H) ones; Anticancer agents; BRCA1 deficient cancer cells; Coupling reactions; PARP 1 inhibitor; Pharmacokinetic properties; SAR exploration

Indexed keywords

5 [(4,5 DIMETHYL 6 OXO 1,6 DIHYDROPYRIDAZIN 3 YL)METHYL] 2 FLUOROBENZOIC ACID; 6 [4 FLUORO 3 (PIPERAZIN 1 YLCARBONYL)BENZYL] 4,5 DIMETHYLPYRIDAZIN 3(2H) ONE; 6 [4 FLUORO 3 [[4 (2 METHYLPROLYL)PIPERAZIN 1 YL]CARBONYL]BENZYL] 4,5 DIMETHYL PYRIDAZIN 3(2H) ONE; ANTINEOPLASTIC AGENT; BRCA1 PROTEIN; CYTOCHROME P450; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE 1; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE INHIBITOR; PIPERAZINE DERIVATIVE; POTASSIUM CHANNEL HERG; PYRIDAZINE DERIVATIVE; UNCLASSIFIED DRUG; BRCA1 PROTEIN, HUMAN; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE; PARP1 PROTEIN, HUMAN;

ANIMAL CELL; ANIMAL CELL CULTURE; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; CYTOTOXICITY; DRUG CLEARANCE; DRUG ELIMINATION; DRUG HALF LIFE; DRUG IDENTIFICATION; HUMAN; HUMAN CELL; HUMAN CELL CULTURE; LIVER MICROSOME; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; URINARY EXCRETION; WILD TYPE; ANIMAL; ANTAGONISTS AND INHIBITORS; COMPARATIVE STUDY; DEFICIENCY; DRUG EFFECTS; ENZYMOLOGY; GENETICS; HELA CELL LINE; METABOLISM; SYNTHESIS;

RATTUS;

ANIMALS; BRCA1 PROTEIN; HELA CELLS; HUMANS; MICROSOMES, LIVER; PIPERAZINES; POLY(ADP-RIBOSE) POLYMERASES; PYRIDAZINES; RATS;

EID: 74049143159     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.11.087     Document Type: Article

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