Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation

Journal of Medicinal Chemistry

Volumn 57, Issue 23, 2014, Pages 10176-10191

  Hanan, Emily J ^a   Eigenbrot, Charles ^a   Bryan, Marian C ^a   Burdick, Daniel J ^a   Chan, Bryan K ^a   Chen, Yuan ^a   Dotson, Jennafer ^a   Heald, Robert A ^b   Jackson, Philip S ^b   La, Hank ^a   Lainchbury, Michael D ^b   Malek, Shiva ^a   Purkey, Hans E ^a   Schaefer, Gabriele ^a   Schmidt, Stephen ^a   Seward, Eileen M ^b   Sideris, Steve ^a   Tam, Christine ^a   Wang, Shumei ^a   Yeap, Siew Kuen ^b   Yen, Ivana ^a   Yin, Jianping ^a   Yu, Christine ^a   Zilberleyb, Inna ^a   Heffron, Timothy P ^a   more..

^a GENENTECH INC   (United States)

^b Argenta Early Discovery Charles River 7 8 Spire Green Centre   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

(1 CYCLOPENTYL 1H PYRROLO[3,2 C ]PYRIDIN 6 YL) [2 (4 METHOXYPIPERIDIN 1 YL)PYRIMIDIN 4 YL]AMINE; (1 ISOPROPYL 1H IMIDAZO[4,5 C ]PYRIDIN 6 YL) [2 (4 METHOXYPIPERIDIN 1 YL)PYRIMIDIN 4 YL]AMINE; (1 ISOPROPYL 1H PYRROLO[3,2 C ]PYRIDIN 6 YL) [2 (4 METHOXYPIPERIDIN 1 YL)PYRIMIDIN 4 YL]AMINE; (2 CHLORO 5 NITROPYRIDIN 4 YL)ISOPROPYLAMINE; 1 ISOPROPYL N [2 (4 METHOXYPIPERIDIN 1 YL)PYRIMIDIN 4 YL] 2 (1H PYRAZOL 4 YL) 1H PYRROLO[3,2 C]PYRIDIN 6 AMINE; 2 (4 METHOXYPIPERIDIN 1 YL)PYRIMIDIN 4 YLAMINE; 2 BROMO 4 CHLORO 5 IODOPYRIDINE; 2 BROMO 5 IODOPYRIDIN 4 AMINE; 6 BROMO 1 ISOPROPYL 1H PYRROLO[3,2 C ]PYRIDINE; 6 BROMO 1 ISOPROPYL 2 [1 [[2 (TRIMETHYLSILYL)ETHOXY]METHYL] 1H PYRAZOL 4 YL] 1H PYRROLO{3,2 C]PYRIDINE; 6 BROMO 1 [[2 (TRIMETHYLSILYL)ETHOXY]METHYL] 2 [1 [[2 (TRIMETHYLSIL)ETHOXY]METHYL] 1H PYRAZOL 4 YL] 1H PYRROLO [3,2 C]PYRIDINE; 6 BROMO 1H PYRAZOLO[4,3 C ]PYRIDINE; 6 BROMO 2 (1H PYRAZOL 4 YL) 1H PYRROLO[3,2 C ]PYRIDINE; 6 BROMO 2 (1H PYRAZOL 4 YL) 3H IMIDAZO[4,5 C ]PYRIDINE; 6 BROMO 2 [1 [[2 (TRIMETHYLSILYL)ETHOXY]METHYL] 1H PYRAZOL 4 YL] 1H PYRROLO[3,2 C ]PYRIDINE; 6 BROMO 3 (2 TRIMETHYLSILANYLETHOXYMETHYL) 2 [1 (2 TRIMETHYLSILANYLETHOXYMETHYL) IH PYRAZOL 4 YL] 3H IMIDAZO[4,5 C]PYRIDINE; 6 BROMO 3 IODO 1 ISOPROPYL 1H PYRAZOLO[4,3 C ]PYRIDINE; 6 BROMO 3 IODO 1H PYRAZOLO[4,3 C ]PYRIDINE; 6 BROMO 4 CHLOROPYRIDINE 3 CARBALDEHYDE; 6 CHLORO 1 CYCLOPENTYL 1H PYRROLO[3,2 C ]PYRIDINE; ANTINEOPLASTIC AGENT; DIAMINOPYRIMIDINE DERIVATIVE; EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; JANUS KINASE 2 INHIBITOR; N (2 BROMO 5 IODOPYRIDIN 4 YL)METHANESULFONAMIDE; N[2 (METHOXYPIPERIDIN 1 YL)PYRIMIDIN 4 YL] 2 (1H PYRAZOL 4 YL) 1H PYRROLO[3,2 C]PYRIDIN 6 AMINE; UNCLASSIFIED DRUG; UNINDEXED DRUG; [2 (4 METHOXYPIPERIDIN 1 YL)PYRIMIDIN 4 YL] [2 (1H PYRAZOL 4 YL) 3H IMIDAZO[4,5 C]PYRIDINE 6 YL]AMINE; AMINOPYRIDINE DERIVATIVE; METHIONINE; PROTEIN KINASE INHIBITOR; THREONINE;

ARTICLE; CELL PROLIFERATION; CELL SURVIVAL; CRYSTAL STRUCTURE; DRUG IDENTIFICATION; DRUG POTENCY; ENZYME INHIBITION; GENE MUTATION; HUMAN; HUMAN TISSUE; NON SMALL CELL LUNG CANCER; PHYSICAL CHEMISTRY; WILD TYPE; X RAY; AMINO ACID SUBSTITUTION; ANTAGONISTS AND INHIBITORS; CARCINOMA, NON-SMALL-CELL LUNG; DRUG RESISTANCE; GENETICS; HIGH THROUGHPUT SCREENING; LUNG NEOPLASMS; MUTATION; SYNTHESIS; X RAY CRYSTALLOGRAPHY;

AMINO ACID SUBSTITUTION; AMINOPYRIDINES; CARCINOMA, NON-SMALL-CELL LUNG; CRYSTALLOGRAPHY, X-RAY; DRUG RESISTANCE, NEOPLASM; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; LUNG NEOPLASMS; METHIONINE; MUTATION; PROTEIN KINASE INHIBITORS; RECEPTOR, EPIDERMAL GROWTH FACTOR; THREONINE;

EID: 84918566121     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm501578n     Document Type: Article

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