Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib

Journal of Medicinal Chemistry

Volumn 56, Issue 3, 2013, Pages 879-894

  Ren, Xiaomei ^a,b   Pan, Xiaofen ^a   Zhang, Zhang ^a   Wang, Deping ^a,c   Lu, Xiaoyun ^a   Li, Yupeng ^a,c   Wen, Donghai ^a   Long, Huoyou ^a   Luo, Jinfeng ^a   Feng, Yubing ^a   Zhuang, Xiaoxi ^a   Zhang, Fengxiang ^a   Liu, Jianqi ^a   Leng, Fang ^a   Lang, Xingfen ^a   Bai, Yang ^a   She, Miaoqin ^a   Tu, Zhengchao ^a   Pan, Jingxuan ^b   Ding, Ke ^a  

^a GUANGZHOU INSTITUTES OF BIOMEDICINE AND HEALTH   (China)

^b SUN YAT SEN UNIVERSITY   (China)

^c UNIVERSITY OF CHINESE ACADEMY OF SCIENCES   (China)

Author keywords

[No Author keywords available]

Indexed keywords

3 [(1H PYRAZOLO[3,4 B]PYRIDIN 5 YL)ETHYNYL] 4 METHYL N [4 [(4 METHYLPIPERAZIN 1 YL)METHYL] 3 (TRIFLUOROMETHYL)PHENYL]BENZAMIDE; ANTINEOPLASTIC AGENT; BCR ABL PROTEIN; BREAKPOINT CLUSTER REGION PROTEIN; GZD 824; IMATINIB; MUTANT PROTEIN; PACLITAXEL; UNCLASSIFIED DRUG;

ACUTE LYMPHOBLASTIC LEUKEMIA; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ANTIPROLIFERATIVE ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CARDIOTOXICITY; CELL PROLIFERATION; CHRONIC MYELOID LEUKEMIA; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CONFORMATION; ENZYME ACTIVITY; HINGE REGION; HUMAN; HUMAN CELL; HYDROGEN BOND; IC 50; IN VIVO STUDY; LEUKEMIA CELL; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; PROTEIN EXPRESSION; PROTEIN PHOSPHORYLATION; SURVIVAL; TIME TO MAXIMUM PLASMA CONCENTRATION; TUMOR REGRESSION; TUMOR VOLUME; TUMOR XENOGRAFT;

ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC AGENTS; BENZAMIDES; BIOLOGICAL AVAILABILITY; CELL LINE, TUMOR; DRUG RESISTANCE, NEOPLASM; FUSION PROTEINS, BCR-ABL; HUMANS; MAGNETIC RESONANCE SPECTROSCOPY; MODELS, MOLECULAR; MUTATION; PHOSPHORYLATION; PIPERAZINES; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES; PYRAZOLES; PYRIMIDINES; SPECTROMETRY, MASS, ELECTROSPRAY IONIZATION;

EID: 84873900689     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm301581y     Document Type: Article

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