Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR)

Journal of Medicinal Chemistry

Volumn 56, Issue 17, 2013, Pages 7025-7048

  Ward, Richard A ^a   Anderton, Mark J ^a   Ashton, Susan ^a   Bethel, Paul A ^a   Box, Matthew ^a   Butterworth, Sam ^a   Colclough, Nicola ^a   Chorley, Christopher G ^a   Chuaqui, Claudio ^a   Cross, Darren A E ^a   Dakin, Les A ^a   Debreczeni, Judit É ^a   Eberlein, Cath ^a   Finlay, M Raymond V ^a   Hill, George B ^a   Grist, Matthew ^a   Klinowska, Teresa C M ^a   Lane, Clare ^a   Martin, Scott ^a   Orme, Jonathon P ^a   Smith, Peter ^a   Wang, Fengjiang ^a   Waring, Michael J ^a   more..

^a ASTRAZENECA   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

3 (2,5 DICHLOROPYRIMIDIN 4 YL) 1H INDOLE; 4 (2 BUTOXYVINYL) 2,5 DICHLORO PYRIMIDINE; 4 FLUORO 2 METHOXY 5 NITROANILINE; 5 CHLORO 4 (1H INDOL 3 YL) N (2 METHOXY 5 NITROPHENYL)PYRIMIDIN 2 AMINE; AFATINIB; CYSTEINE; DACOMITINIB; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; GEFITINIB; MUTANT PROTEIN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIPROLIFERATIVE ACTIVITY; ARTICLE; BINDING SITE; CANCER INHIBITION; COMPARATIVE STUDY; CONFORMATION; CONTROLLED STUDY; COVALENT BOND; CRYSTAL STRUCTURE; CRYSTALLIZATION; CYCLIZATION; DRUG EFFICACY; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; ELECTROPHILICITY; HUMAN; HUMAN CELL; IC 50; LIPOPHILICITY; LIQUID CHROMATOGRAPHY; MASS SPECTROMETRY; MOLECULAR MODEL; MOUSE; NITRATION; NONHUMAN; PHYSICAL CHEMISTRY; QUANTITATIVE STRUCTURE PROPERTY RELATION; WILD TYPE;

MODELS, MOLECULAR; MUTATION; RECEPTOR, EPIDERMAL GROWTH FACTOR; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84884243421     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm400822z     Document Type: Article

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