Optimization of phenyl-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase inhibitors: Identification of (S)-2-(2-fluoro-4- (pyrrolidin-2-yl)phenyl)-1 H -benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious inhibitor

Journal of Medicinal Chemistry

Volumn 53, Issue 8, 2010, Pages 3142-3153

  Penning, Thomas D ^a   Zhu, Gui Dong ^a   Gong, Jianchun ^a   Thomas, Sheela ^a   Gandhi, Viraj B ^a   Liu, Xuesong ^a   Shi, Yan ^a   Klinghofer, Vered ^a   Johnson, Eric F ^a   Park, Chang H ^a   Fry, Elizabeth H ^a   Donawho, Cherrie K ^a   Frost, David J ^a   Buchanan, Fritz G ^a   Bukofzer, Gail T ^a   Rodriguez, Luis E ^a   Bontcheva Diaz, Velitchka ^a   Bouska, Jennifer J ^a   Osterling, Donald J ^a   Olson, Amanda M ^a   Marsh, Kennan C ^a   Luo, Yan ^a   Giranda, Vincent L ^a   more..

^a ABBOTT LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 [2 FLUORO 4 (PYRROLIDIN 2 YL)PHENYL] 1H BENZIMIDAZOLE 4 CARBOXAMIDE; A 966492; AMIDE; BENZIMIDAZOLE DERIVATIVE; CARBOPLATIN; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE INHIBITOR; PHENYL GROUP; TEMOZOLOMIDE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; BLOOD BRAIN BARRIER; BREAST CANCER; CELL ASSAY; CONCENTRATION RESPONSE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DOG; DRUG EFFICACY; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG POTENCY; DRUG SYNTHESIS; ENZYME INHIBITION; MAXIMUM PLASMA CONCENTRATION; MELANOMA; MELANOMA B16; MONKEY; MOUSE; NONHUMAN; TREATMENT OUTCOME; TREATMENT RESPONSE; TUMOR VOLUME; TUMOR XENOGRAFT; WHOLE CELL;

ANIMALS; ANTINEOPLASTIC AGENTS; ANTINEOPLASTIC COMBINED CHEMOTHERAPY PROTOCOLS; BENZIMIDAZOLES; BIOLOGICAL AVAILABILITY; BLOOD-BRAIN BARRIER; BRCA1 PROTEIN; CARBOPLATIN; CELL LINE, TUMOR; CRYSTALLOGRAPHY, X-RAY; DACARBAZINE; DRUG SCREENING ASSAYS, ANTITUMOR; FEMALE; MELANOMA, EXPERIMENTAL; MICE; MICE, INBRED C57BL; MICE, SCID; MODELS, MOLECULAR; NEOPLASM TRANSPLANTATION; POLY(ADP-RIBOSE) POLYMERASES; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSPLANTATION, HETEROLOGOUS;

EID: 77951110744     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm901775y     Document Type: Article

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