Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity

Journal of Medicinal Chemistry

Volumn 48, Issue 4, 2005, Pages 1107-1131

  Tsou, Hwei Ru ^a   Overbeek Klumpers, Elsebe G ^a   Hallett, William A ^a   Reich, Marvin F ^a   Floyd, M Brawner ^a   Johnson, Bernard D ^a   Michalak, Ronald S ^a   Nilakantan, Ramaswamy ^a   Discafani, Carolyn ^a   Golas, Jonathan ^a   Rabindran, Sridhar K ^a   Shen, Ru ^a   Shi, Xiaoqing ^a   Wang, Yu Fen ^a   Upeslacis, Janis ^a   Wissner, Allan ^a  

^a WYETH RESEARCH   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 ANILINOQUINOLINE 3 CARBONITRILE DERIVATIVE; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; HKI 272; N [4 (4 BENZYLOXY 3 CHLOROPHENYLAMINE) 3 CYANO 7 ETHOXY 6 QUINOLINYL] 4 (DIMETHYLAMINO) 2 BUTENAMIDE; N [4 [3 CHLORO 4 (2 NAPHTHYLMETHOXY)ANILINO] 3 CYANO 7 ETHOXY 6 QUINOLYL] 4 (DIMETHYLAMINO) 2 BUTENAMIDE; N [4 [3 CHLORO 4 (2 THIENYLMETHOXY)ANILINO] 3 CYANO 7 ETHOXY 6 QUINOLINYL] 4 (DIMETHYLAMINO) 2 BUTENAMIDE; N [4 [3 CHLORO 4 (3 FLUOROBENZYLOXY)PHENYLAMINO] 3 CYANO 7 ETHOXY 6 QUINOLYL](DIMETHYLAMINO) 2 BUTENAMIDE; N [4 [4 (BENZYLOXY) 3 CHLOROANILINO] 3 CYANO 7 ETHOXY 6 QUINOLINYL] 4 (1 PIPERIDINYL) 2 BUTENAMIDE; N [4 [4 (BENZYLOXY) 3 CHLOROANILINO] 3 CYANO 7 ETHOXY 6 QUINOLINYL] 4 (PYRROLIDIN 1 YL) 2 BUTENAMIDE; PELITINIB; UNCLASSIFIED DRUG;

ACYLATION; AMINATION; ANIMAL CELL; ANIMAL MODEL; ARTICLE; BINDING KINETICS; CANCER; CONTROLLED STUDY; CYCLIZATION; DRUG ACTIVITY; DRUG POTENCY; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; INHIBITION KINETICS; LIPOPHILICITY; MICHAEL ADDITION; MOLECULAR MODEL; MOUSE; NONHUMAN; REACTION OPTIMIZATION; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC AGENTS; BINDING SITES; CELL LINE, TUMOR; CELL PROLIFERATION; DRUG SCREENING ASSAYS, ANTITUMOR; FEMALE; HUMANS; MICE; MICE, NUDE; MODELS, MOLECULAR; NITRILES; PHOSPHORYLATION; PROTEIN BINDING; QUINOLINES; RADIOLIGAND ASSAY; RECEPTOR, EPIDERMAL GROWTH FACTOR; RECEPTOR, ERBB-2; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSPLANTATION, HETEROLOGOUS;

EID: 13944262091     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm040159c     Document Type: Article

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