Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-Methylpropyl)-12, 13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4 H -indazolo[5,4-a]pyrrolo[3,4-c] carbazol-4-one (CEP-11981): A novel oncology therapeutic agent

Journal of Medicinal Chemistry

Volumn 55, Issue 2, 2012, Pages 903-913

  Hudkins, Robert L ^a   Becknell, Nadine C ^a   Zulli, Allison L ^a   Underiner, Ted L ^a   Angeles, Thelma S ^a   Aimone, Lisa D ^a   Albom, Mark S ^a   Chang, Hong ^a   Miknyoczki, Sheila J ^a   Hunter, Kathryn ^a   Jones Bolin, Susan ^a   Zhao, Hugh ^a   Bacon, Edward R ^a   Mallamo, John P ^a   Ator, Mark A ^a   Ruggeri, Bruce A ^a  

^a CEPHALON INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

11 (1 METHYLETHYL) 12,13 DIHYDRO 2 METHYL 8 (PYRIMIDIN 2 YLAMINO) 4H INDAZOLO[5,4 A]PYRROLO[3,4 C]CARBAZOL 4 ONE; 11 (2 METHYLETHYL) 12,13 DIHYDRO 2 METHYL 8 (3 PYRIDAZINYLAMINO) 4H INDAZOLO[5,4 A]PYRROLO[3,4 C]CARBAZOL 4 ONE; 11 (2 METHYLETHYL) 12,13 DIHYDRO 2 METHYL 8 (4 PYRIDINYLAMINO) 4H INDAZOLO[5,4 A]PYRROLO[3,4 C]CARBAZOL 4 ONE; 11 (2 METHYLPROPYL) 12,13 DIHYDRO 2 METHYL 8 (4 METHOXYPYRIMIDIN 2 YLAMINO) 4H INDAZOLO[5,4 A]PYRROLO[3,4 C]CARBAZOL 4 ONE; 11 (2 METHYLPROPYL) 12,13 DIHYDRO 2 METHYL 8 (4 TRIFLUOROMETHYL PYRIMIDIN 2 YLAMINO) 4H INDAZOLO[5,4 A]PYRROLO[3,4 C]CARBAZOL 4 ONE; 11 (2 METHYLPROPYL) 12,13 DIHYDRO 2 METHYL 8 (4,6 DIMETHYLPYRIMIDIN 2 YLAMINO) 4H INDAZOLO[5,4 A]PYRROLO[3,4 C]CARBAZOL 4 ONE; 11 (2 METHYLPROPYL) 12,13 DIHYDRO 2 METHYL 8 (5 ETHYLPYRIETHYLPYRIMIDIN 2 YLAMINO) 4H INDAZOLO[5,4 A]PYRROLO[3,4 C]CARBAZOL 4 ONE; 11 (2 METHYLPROPYL) 12,13 DIHYDRO 2 METHYL 8 (PYRIMIDIN 2 YLAMINO) 4H INDAZOLO[5,4 A]PYRROLO[3,4 C]CARBAZOL 4 ONE; 11 PROPYL 12,13 DIHYDRO 2 METHYL 8 (5 ETHYL PYRIMIDIN 2 YLAMINO) 4H INDAZOLO[5,4 A]PYRROLO[3,4 C]CARBAZOL 4 ONE; 11 PROPYL 12,13 DIHYDRO 2 METHYL 8 (PYRIMIDIN 2 YLAMINO) 4H INDAZOLO[5,4 A]PYRROLO[3,4 C]CARBAZOL 4 ONE; ANGIOPOIETIN RECEPTOR; ANTINEOPLASTIC AGENT; CEP 11981; FIBROBLAST GROWTH FACTOR RECEPTOR 1; UNCLASSIFIED DRUG; VASCULOTROPIN INHIBITOR; VASCULOTROPIN RECEPTOR 1; VASCULOTROPIN RECEPTOR 2; VASCULOTROPIN RECEPTOR 3;

ANGIOGENESIS; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTINEOPLASTIC ACTIVITY; ARTICLE; BIOCHEMICAL COMPOSITION; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG DOSE ESCALATION; DRUG HALF LIFE; DRUG SAFETY; DRUG SYNTHESIS; FEMALE; HUMAN; HUMAN CELL; IC 50; MALE; MOLECULAR MODEL; NONHUMAN; PHASE 1 CLINICAL TRIAL (TOPIC); RAT; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANGIOGENESIS INHIBITORS; ANIMALS; BIOLOGICAL AVAILABILITY; CARBAZOLES; HUMANS; INDAZOLES; MACACA FASCICULARIS; MALE; MICE; MICE, NUDE; MODELS, MOLECULAR; NEOVASCULARIZATION, PHYSIOLOGIC; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, FIBROBLAST GROWTH FACTOR, TYPE 1; RECEPTOR, TIE-2; RECEPTORS, VASCULAR ENDOTHELIAL GROWTH FACTOR; RECOMBINANT PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP; VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR-1; VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR-2; VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR-3; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84863080201     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm201449n     Document Type: Article

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