Discovery, design, and synthesis of indole-based EZH2 inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 25, Issue 17, 2015, Pages 3644-3649

  Gehling, Victor S ^a   Vaswani, Rishi G ^a   Nasveschuk, Christopher G ^a   Duplessis, Martin ^a   Iyer, Priyadarshini ^a   Balasubramanian, Srividya ^a   Zhao, Feng ^a   Good, Andrew C ^a   Campbell, Robert ^a   Lee, Christina ^a   Dakin, Les A ^a   Cook, Andrew S ^a   Gagnon, Alexandre ^a   Harmange, Jean Christophe ^a   Audia, James E ^a   Cummings, Richard T ^a   Normant, Emmanuel ^a   Trojer, Patrick ^a   Albrecht, Brian K ^a  

^a Department of Lead Discovery   (United States)

Author keywords

Epigenetics; EZH2; Histone methyltransferase; PRC2; Pyridone

Indexed keywords

INDOLE DERIVATIVE; SULFONAMIDE; TRANSCRIPTION FACTOR EZH2; TRANSCRIPTION FACTOR EZH2 INHIBITOR; UNCLASSIFIED DRUG; ANTINEOPLASTIC AGENT; EZH2 PROTEIN, HUMAN; INDOLE; MOLECULAR LIBRARY; POLYCOMB REPRESSIVE COMPLEX 2;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DRUG DESIGN; DRUG DEVELOPMENT; DRUG POTENCY; DRUG STABILITY; DRUG SYNTHESIS; EC50; IC50; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION; TUMOR XENOGRAFT; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DRUG EFFECTS; DRUG SCREENING; HELA CELL LINE; HUMAN; MOLECULAR LIBRARY; MOLECULARLY TARGETED THERAPY; PHARMACOLOGY; PROCEDURES; SYNTHESIS; TUMOR CELL LINE;

ANIMALS; ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; CHEMISTRY TECHNIQUES, SYNTHETIC; DRUG DESIGN; DRUG DISCOVERY; DRUG SCREENING ASSAYS, ANTITUMOR; DRUG STABILITY; HELA CELLS; HUMANS; INDOLES; INHIBITORY CONCENTRATION 50; MICE; MOLECULAR TARGETED THERAPY; POLYCOMB REPRESSIVE COMPLEX 2; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84938375449     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2015.06.056     Document Type: Article

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