Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: Design, synthesis, and biological evaluation of C -7-substituted 1,3-benzothiazole derivatives

Journal of Medicinal Chemistry

Volumn 56, Issue 16, 2013, Pages 6478-6494

  Okaniwa, Masanori ^a   Hirose, Masaaki ^a   Arita, Takeo ^a   Yabuki, Masato ^a   Nakamura, Akito ^a   Takagi, Terufumi ^a   Kawamoto, Tomohiro ^a   Uchiyama, Noriko ^a   Sumita, Akihiko ^a   Tsutsumi, Shunichirou ^a   Tottori, Tsuneaki ^a   Inui, Yoshitaka ^a   Sang, Bi Ching ^b   Yano, Jason ^b   Aertgeerts, Kathleen ^b   Yoshida, Sei ^a   Ishikawa, Tomoyasu ^a  

^a TAKEDA PHARMACEUTICAL COMPANY LIMITED   (Japan)

^b Takeda San Diego Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; B RAF KINASE; BENZOTHIAZOLE DERIVATIVE; N [7 CYANO 6 [4 FLUORO 3 [[[3 (TRIFLUOROMETHYL)PHENYL]ACETYL]AMINO]PHENOXY] 1,3 BENZOTHIAZOL 2 YL]CYCLOPROPANECARBOXAMIDE; PHOSPHOTRANSFERASE INHIBITOR; PYRIDINE DERIVATIVE; RAF PROTEIN; TAK 632; UNCLASSIFIED DRUG; VASCULOTROPIN RECEPTOR 2;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BIOLOGICAL ACTIVITY; BODY WEIGHT; CANCER CELL CULTURE; CONTROLLED STUDY; CRYSTAL STRUCTURE; CYCLIZATION; DOG; DOSE RESPONSE; DRUG ABSORPTION; DRUG ACTIVITY; DRUG BINDING; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG EFFECT; DRUG MECHANISM; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HYDROPHOBICITY; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; TUMOR XENOGRAFT;

BENZOTHIAZOLES; BLOOD-BRAIN BARRIER; CELL LINE, TUMOR; CRYSTALLOGRAPHY, X-RAY; DRUG DISCOVERY; DRUG EVALUATION, PRECLINICAL; HUMANS; MODELS, MOLECULAR; PROTEIN KINASE INHIBITORS; SURFACE PLASMON RESONANCE;

EID: 84883173554     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm400778d     Document Type: Article

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