Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl) benzamide derivatives as potent pan Bcr-Abl inhibitors including the threonine315←isoleucine315 mutant

Journal of Medicinal Chemistry

Volumn 55, Issue 22, 2012, Pages 10033-10046

  Li, Yupeng ^a,b   Shen, Mengjie ^a,b   Zhang, Zhang ^a   Luo, Jinfeng ^a   Pan, Xiaofen ^a   Lu, Xiaoyun ^a   Long, Huoyou ^a   Wen, Donghai ^a   Zhang, Fengxiang ^a   Leng, Fang ^a   Li, Yingjun ^a,b   Tu, Zhengchao ^a   Ren, Xiaomei ^a   Ding, Ke ^a  

^a GUANGZHOU INSTITUTES OF BIOMEDICINE AND HEALTH   (China)

^b UNIVERSITY OF CHINESE ACADEMY OF SCIENCES   (China)

Author keywords

[No Author keywords available]

Indexed keywords

3 ( 4 ( 1H PYRAZOLO[3,4 B]PYRIDIN 5 YL) 1H 1,2,3 TRIAZOL 1 YL) 4 CYCLOPROPYL N ( 4 (( 4 METHYLPIPERAZIN 1 YL)METHYL) 3 (TRIFLUOROMETHYL)PHENYL)BENZAMIDE; 3 ( 4 ( 1H PYRAZOLO[3,4 B]PYRIDIN 5 YL) 1H 1,2,3 TRIAZOL 1 YL) 4 METHYL N ( 3 ( 4 METHYL 1H IMIDAZOL 1 YL) 5 (TRIFLUOROMETHYL)PHENYL)BENZAMIDE; 3 ( 4 ( 1H PYRAZOLO[3,4 B]PYRIDIN 5 YL) 1H 1,2,3 TRIAZOL 1 YL) 4 METHYL N ( 4 (( 4 METHYL 1,4 DIAZEPAN 1 YL)METHYL) 3 (TRIFLUOROMETHYL)PHENYL)BENZAMIDE; 3 ( 4 ( 1H PYRAZOLO[3,4 B]PYRIDIN 5 YL) 1H 1,2,3 TRIAZOL 1 YL) 4 METHYL N ( 4 (( 4 METHYLPIPERAZIN 1 YL)METHYL) 3 (TRIFLUOROMETHYLPHENYL)BENZAMIDE; ANTINEOPLASTIC AGENT; BAFETINIB; BCR ABL PROTEIN; BENZAMIDE DERIVATIVE; BOSUTINIB; DASATINIB; GNF 7; IMATINIB; ISOLEUCINE; NILOTINIB; PONATINIB; PROTEIN KINASE; PROTEIN TYROSINE KINASE INHIBITOR; REBASTINIB; THREONINE; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; ANIMAL CELL; ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER RESISTANCE; CELL PROLIFERATION; CHRONIC MYELOID LEUKEMIA; COMBINATORIAL CHEMISTRY; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG CONFORMATION; DRUG DESIGN; DRUG POTENCY; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME INHIBITION; GENE EXPRESSION; GENE MUTATION; HUMAN; HUMAN CELL; IC 50; LEUKEMIA CELL; LEUKEMIA CELL LINE; MUTANT; NONHUMAN; WILD TYPE;

BENZAMIDES; BLOTTING, WESTERN; CELL LINE, TUMOR; CELL PROLIFERATION; CELLS, CULTURED; DRUG DESIGN; DRUG RESISTANCE, NEOPLASM; FUSION PROTEINS, BCR-ABL; HUMANS; ISOLEUCINE; LEUKEMIA, MYELOGENOUS, CHRONIC, BCR-ABL POSITIVE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; MUTATION; PHOSPHORYLATION; PIPERAZINES; PROTEIN KINASE INHIBITORS; PYRIMIDINES; STRUCTURE-ACTIVITY RELATIONSHIP; THREONINE;

EID: 84870003659     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm301188x     Document Type: Article

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