Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor

Journal of Medicinal Chemistry

Volumn 58, Issue 20, 2015, Pages 8200-8215

  Zeng, Qingbei ^a   Wang, Jiabing ^a   Cheng, Ziqiang ^a   Chen, Kan ^a   Johnström, Peter ^b   Varnäs, Katarina ^b   Li, David Yunzhi ^a   Yang, Zhen Fan ^a   Zhang, Xiaolin ^a  

^a ASTRAZENECA   (United Kingdom)

^b KAROLINSKA UNIVERSITY HOSPITAL   (Sweden)

Author keywords

[No Author keywords available]

Indexed keywords

4 [(3 CHLORO 2 FLUOROPHENYL)AMINO] 7 METHOXYQUINAZOLIN 6 YL 2,4 DIMETHYLPIPERAZINE 1 CARBOXYLATE; EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; UNCLASSIFIED DRUG; AZD3759; PIPERAZINE DERIVATIVE; PROTEIN KINASE INHIBITOR; PROTEIN TYROSINE KINASE; QUINAZOLINE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BRAIN METASTASIS; CENTRAL NERVOUS SYSTEM; DOG; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DESIGN; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG PENETRATION; DRUG POTENCY; DRUG SCREENING; DRUG SYNTHESIS; HUMAN; HUMAN CELL; MACACA FASCICULARIS; MALE; MOUSE; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; VOLUME OF DISTRIBUTION AT STEADY-STATE; ANIMAL; ANTAGONISTS AND INHIBITORS; BRAIN; BRAIN NEOPLASMS; DRUG DEVELOPMENT; METABOLISM; PHASE 1 CLINICAL TRIAL (TOPIC); POSITRON EMISSION TOMOGRAPHY; SCINTISCANNING; SECONDARY; SYNTHESIS; WISTAR RAT;

ANIMALS; BRAIN; BRAIN NEOPLASMS; CENTRAL NERVOUS SYSTEM; CLINICAL TRIALS, PHASE I AS TOPIC; DOGS; DRUG DISCOVERY; MACACA FASCICULARIS; MALE; MICE; PIPERAZINES; POSITRON-EMISSION TOMOGRAPHY; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES; QUINAZOLINES; RATS; RATS, WISTAR; RECEPTOR, EPIDERMAL GROWTH FACTOR; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84945325367     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b01073     Document Type: Article

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