Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression

Journal of Medicinal Chemistry

Volumn 61, Issue 2, 2018, Pages 462-481

  Zhou, Bing ^a,b   Hu, Jiantao ^a,b   Xu, Fuming ^a,b   Chen, Zhuo ^a,b   Bai, Longchuan ^a,b   Fernandez Salas, Ester ^a   Lin, Mei ^a,b   Liu, Liu ^a,b   Yang, Chao Yie ^a,b   Zhao, Yujun ^a,b   McEachern, Donna ^a,b   Przybranowski, Sally ^a,b   Wen, Bo ^a   Sun, Duxin ^a   Wang, Shaomeng ^a,b  

^a UNIVERSITY OF MICHIGAN   (United States)

^b UNIVERSITY OF MICHIGAN MEDICAL SCHOOL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 [(3 CYCLOPROPYL 1 ETHYL 1H PYRAZOL 5 YL)AMINO] 7 (3,5 DIMETHYLISOXAZOL 4 YL) N[5 [2 (2,6 DIOXOPIPERIDIN 3 YL) 1 OXOISOINDOLIN 4 YL]PENTYL] 6 METHOXY 9H PYRIMIDO[4,5]B INDOLE 2 CARBOXAMIDE; BROMODOMAIN INHIBITOR; UNCLASSIFIED DRUG; ANTINEOPLASTIC AGENT; BRD2 PROTEIN, HUMAN; BRD3 PROTEIN, HUMAN; BRD4 PROTEIN, HUMAN; INDOLE DERIVATIVE; NUCLEAR PROTEIN; PROTEIN SERINE THREONINE KINASE; PYRIMIDINE DERIVATIVE; RNA BINDING PROTEIN; TRANSCRIPTION FACTOR;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CANCER REGRESSION; CELL GROWTH; CHIMERA; CONTROLLED STUDY; DRUG DESIGN; DRUG POTENCY; DRUG SYNTHESIS; FEMALE; HUMAN; HUMAN CELL; IC50; MOUSE; NONHUMAN; PROTEIN DEGRADATION; PROTEIN TARGETING; RS4 11 CELL LINE; ANIMAL; CHEMISTRY; DOSE RESPONSE; DRUG SCREENING; LEUKEMIA; METABOLISM; MOLECULAR LIBRARY; PHARMACOLOGY; PROCEDURES; SCID MOUSE; STRUCTURE ACTIVITY RELATION; SYNTHESIS; TUMOR CELL LINE;

ANIMALS; ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; DRUG SCREENING ASSAYS, ANTITUMOR; FEMALE; HUMANS; INDOLES; LEUKEMIA; MICE, SCID; NUCLEAR PROTEINS; PROTEIN-SERINE-THREONINE KINASES; PROTEOLYSIS; PYRIMIDINES; RNA-BINDING PROTEINS; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSCRIPTION FACTORS; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 85041102317     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.6b01816     Document Type: Article

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