Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib

Journal of Medicinal Chemistry

Volumn 57, Issue 6, 2014, Pages 2692-2703

  Cheng, Huimin ^a   Chang, Yu ^b   Zhang, Lianwen ^a   Luo, Jinfeng ^a   Tu, Zhengchao ^a   Lu, Xiaoyun ^a   Zhang, Qingwen ^b   Lu, Jibu ^c   Ren, Xiaomei ^a   Ding, Ke ^a  

^a GUANGZHOU INSTITUTES OF BIOMEDICINE AND HEALTH   (China)

^b UNIVERSITY OF MACAU   (Macao)

^c SHENYANG PHARMACEUTICAL UNIVERSITY   (China)

Author keywords

[No Author keywords available]

Indexed keywords

1H PYRAZOLO[3,4 B]PYRIDINE 5 CARBOXAMIDE DERIVATIVE; ANTINEOPLASTIC AGENT; B RAF KINASE; B RAF KINASE INHIBITOR; EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; MITOGEN ACTIVATED PROTEIN KINASE; N [2 METHYL 5 [[4 [(4 METHYLPIPERAZIN 1 YL)METHYL] 3 (TRIFLUOROMETHYL)PHENYL]CARBAMOYL] PHENYL] 1H PYRROLO[2,3 B]PYRIDINE 5 CARBOXAMIDE; UNCLASSIFIED DRUG; VEMURAFENIB;

ANTIPROLIFERATIVE ACTIVITY; ARTICLE; CANCER CELL CULTURE; CANCER RESISTANCE; CELL PROLIFERATION; COLORECTAL CANCER; CONTROLLED STUDY; DRUG MECHANISM; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME ACTIVATION; ENZYME INHIBITION; HUMAN; HUMAN CELL; IC 50; MELANOMA; PROTEIN EXPRESSION; STRUCTURE ACTIVITY RELATION;

BLOTTING, WESTERN; CELL LINE, TUMOR; CELL PROLIFERATION; COLORECTAL NEOPLASMS; DRUG EVALUATION, PRECLINICAL; DRUG RESISTANCE, NEOPLASM; GENES, ERBB-1; HUMANS; INDICATORS AND REAGENTS; INDOLES; MELANOMA; MITOGEN-ACTIVATED PROTEIN KINASES; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS B-RAF; RECEPTOR, EPIDERMAL GROWTH FACTOR; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES;

EID: 84897407253     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm500007h     Document Type: Article

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