Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor

Journal of Medicinal Chemistry

Volumn 53, Issue 17, 2010, Pages 6368-6377

  Cee, Victor J ^a   Schenkel, Laurie B ^a   Hodous, Brian L ^a   Deak, Holly L ^a   Nguyen, Hanh N ^a   Olivieri, Philip R ^a   Romero, Karina ^a   Bak, Annette ^a   Be, Xuhai ^a   Bellon, Steve ^a   Bush, Tammy L ^a   Cheng, Alan C ^a   Chung, Grace ^a   Coats, Steve ^a   Eden, Patrick M ^a   Hanestad, Kelly ^a   Gallant, Paul L ^a   Gu, Yan ^a   Huang, Xin ^a   Kendall, Richard L ^a   Lin, Min Hwa Jasmine ^a   Morrison, Michael J ^a   Patel, Vinod F ^a   Radinsky, Robert ^a   Rose, Paul E ^a   Ross, Sandra ^a   Sun, Ji Rong ^a   Tang, Jin ^a   Zhao, Huilin ^a   Payton, Marc ^a   Geuns Meyer, Stephanie D ^a   more..

^a AMGEN INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 AMINOBENZAMIDE; 2 CHLORO N (3 METHYL 4 (3 (2 (METHYLAMINO)PYRIMIDIN 4 YL) PYRIDIN 2 YLOXY)PHENYL)BENZAMIDE; 2 CHLORO N (3 METHYL 4 (3 (2 (METHYLAMINO)PYRIMIDIN 4 YL)PYRIDIN 2 YLOXY)PHENYL)BENZAMIDE; 3 CHLORO N (3 METHYL 4 (3 (2 (METHYLAMINO)PYRIMIDIN 4 YL) PYRIDIN 2 YLOXY)PHENYL)BENZAMIDE; 3 CHLORO N (3 METHYL 4 (3 (2 (METHYLAMINO)PYRIMIDIN 4 YL)PYRIDIN 2 YLOXY)PHENYL)BENZAMIDE; 4 (2 (4 AMINO 2 METHYLPHENOXY)PYRIDINE 3 YL) N METHYLPYRIMIDIN 2 AMINE; 4 (2 (4 AMINOPHENOXY)PYRIDIN 3 YL) N METHYLPYRIMIDIN 2 AMINE; 4 (4 FLUOROPHENYL) N (4 (3 (2 (METHYLAMINO)PYRIMIDIN 4 YL)PYRIDIN 2 YLOXY)PHENYL)PHTHALAZIN 1 AMINE; 4 CHLORO N (3 METHYL 4 (3 (2 (METHYLAMINO)PYRIMIDIN 4 YL) PYRIDIN 2 YLOXY)PHENYL)BENZAMIDE; 4 CHLORO N (3 METHYL 4 (3 (2 (METHYLAMINO)PYRIMIDIN 4 YL)PYRIDIN 2 YLOXY)PHENYL)BENZAMIDE; 4 CHLORO N (4 (3 (2 (METHYLAMINO)PYRIMIDIN 4 YL)PYRIDIN 2 YLOXY)PHENYL)PHTHALAZIN 1 AMINE; 5 FLUORO N (4 (3 (2 (METHYLAMINO)PYRIMIDIN 4 YL)PYRIDIN 2 YLOXY)PHENYL) 2 (PHENYLAMINO)BENZAMIDE; AURORA KINASE INHIBITOR; HISTONE H3; N (2 METHYL 4 (3 (2 (METHYLAMINO)PYRIMIDIN 4 YL)PYRIDIN 2 YLOXY)PHENYL) 2 (PHENYLAMINO)BENZAMIDE; N (3 METHYL 4 (3 (2 (METHYLAMINO)PYRIMIDIN 4 YL)PYRIDIN 2 AMINE; N (3 METHYL 4 (3 (2 (METHYLAMINO)PYRIMIDIN 4 YL)PYRIDIN 2 YLOXY)PHENYL) 2 (PHENYLAMINO)BENZAMIDE; N (3 METHYL 4 (3 (2 (METHYLAMINO)PYRIMIDIN 4 YL)PYRIDIN 2 YLOXY)PHENYL) 2 PHENOXYBENZAMIDE; N (3 METHYL 4 (3 (2 (METHYLAMINO)PYRIMIDIN 4 YL)PYRIDIN 2 YLOXY)PHENYL) 3 (TRIFLUOROMETHYL)BENZAMIDE; N (3 METHYL 4 (3 (2 (METHYLAMINO)PYRIMIDIN 4 YL)PYRIDIN 2 YLOXY)PHENYL) 4 PHENOXYBENZAMIDE; N (4 (3 (2 (METHYLAMINO)PYRIMIDIN 4 YL)PYRIDIN 2 YLOXY)PHENYL) 2 (PHENYLAMINO)BENZAMIDE; N (4 (3 (2 (METHYLAMINO)PYRIMIDIN 4 YL)PYRIDIN 2 YLOXY)PHENYL) 4 PHENYLPHTHALAZIN 1 AMINE; PHTHALAZINE DERIVATIVE; PYRIDINYL PYRIMIDINE; UNCLASSIFIED DRUG;

ARTICLE; CELL ACTIVITY; DRUG MECHANISM; DRUG STRUCTURE; ENZYME ACTIVITY; HYDROGEN BOND; PROTEIN PHOSPHORYLATION;

ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC AGENTS; BIOLOGICAL AVAILABILITY; BLOOD PROTEINS; CELL LINE, TUMOR; DRUG SCREENING ASSAYS, ANTITUMOR; FEMALE; HISTONES; HUMANS; MALE; MICE; MICE, NUDE; MICROSOMES, LIVER; MODELS, MOLECULAR; NEOPLASM TRANSPLANTATION; PHTHALAZINES; PROTEIN BINDING; PROTEIN-SERINE-THREONINE KINASES; PYRIDINES; PYRIMIDINES; RATS; RATS, SPRAGUE-DAWLEY; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSPLANTATION, HETEROLOGOUS;

EID: 77956320877     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm100394y     Document Type: Article

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