Discovery and optimization of a novel series of potent mutant B-Raf V600E selective kinase inhibitors

Journal of Medicinal Chemistry

Volumn 56, Issue 5, 2013, Pages 1996-2015

  Vasbinder, Melissa M ^a   Aquila, Brian ^a   Augustin, Martin ^b   Chen, Huawei ^a   Cheung, Tony ^a   Cook, Donald ^a   Drew, Lisa ^a   Fauber, Benjamin P ^a,c   Glossop, Steve ^a   Grondine, Michael ^a   Hennessy, Edward ^a   Johannes, Jeffrey ^a   Lee, Stephen ^a   Lyne, Paul ^a   Mörtl, Mario ^b   Omer, Charles ^a   Palakurthi, Sangeetha ^a,d   Pontz, Timothy ^a   Read, Jon ^a   Sha, Li ^a   Shen, Minhui ^a   Steinbacher, Stefan ^b   Wang, Haixia ^a   Wu, Allan ^a   Ye, Minwei ^a   more..

^a ASTRAZENECA   (United Kingdom)

^b PROTEROS BIOSTRUCTURES GMBH   (Germany)

^c GENENTECH INC   (United States)

^d HARVARD INSTITUTES OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 (1 (4 (6 (PYRIDIN 4 YL)QUINAZOLIN 2 YLAMINO)PHENYL)ETHYLAMINO)CYCLOHEX 2 ENONE; ACETAMIDE DERIVATIVE; AMIDE; B RAF KINASE INHIBITOR; BENZAMIDE DERIVATIVE; MITOGEN ACTIVATED PROTEIN KINASE; N (1 (4 (6 (PYRIDIN 4 YL)QUINAZOLIN 2 YLAMINO)PHENYL)ETHYL)ACETAMIDE; N (1 (4 (6 (PYRIDIN 4 YL)QUINAZOLIN 2 YLAMINO)PHENYL)ETHYL)PIPERIDINE 2 CARBOXAMIDE HYDROCHLORIDE; N (1 (4 (8 METHOXY 6 (PYRIDIN 4 YL)QUINAZOLIN 2 YLAMINO)PHENYL)ETHYL)ACETAMIDE; N (2 METHOXYETHYL) 4 [(6 PYRIDIN 4 YLQUINAZOLIN 2 YL) AMINO]BEZAMIDE; N (2,3 DIHYDROXYPROPOXY) 3,4 DIFLUORO 2 (2 FLUORO 4 IODOANILINO)BENZAMIDE; N METHYL N {4 [(6 PYRIDIN 4 YLQUINAZOLIN 2 YL)AMINO]PHENYL}ACETAMIDE; UNCLASSIFIED DRUG;

ANTIPROLIFERATIVE ACTIVITY; ARTICLE; CANCER INHIBITION; DRUG BINDING; DRUG DOSE INCREASE; DRUG EFFICACY; DRUG SOLUBILITY; DRUG TOLERABILITY; METASTATIC MELANOMA; XENOGRAFT;

ANIMALS; HUMANS; MALE; MELANOMA; MICE; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS B-RAF; QUINAZOLINES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84875191732     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm301658d     Document Type: Article

References (35)

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