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Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas.
Vaswani, Rishi G; Gehling, Victor S; Dakin, Les A; Cook, Andrew S; Nasveschuk, Christopher G; Duplessis, Martin; Iyer, Priyadarshini; Balasubramanian, Srividya; Zhao, Feng; Good, Andrew C; Campbell, Robert; Lee, Christina; Cantone, Nico; Cummings, Richard T; Normant, Emmanuel; Bellon, Steven F; Albrecht, Brian K; Harmange, Jean-Christophe; Trojer, Patrick; Audia, James E; Zhang, Ying; Justin, Neil; Chen, Shuyang; Wilson, Jon R; Gamblin, Steven J.
Affiliation
  • Vaswani RG; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Gehling VS; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Dakin LA; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Cook AS; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Nasveschuk CG; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Duplessis M; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Iyer P; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Balasubramanian S; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Zhao F; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Good AC; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Campbell R; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Lee C; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Cantone N; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Cummings RT; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Normant E; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Bellon SF; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Albrecht BK; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Harmange JC; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Trojer P; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Audia JE; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Zhang Y; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Justin N; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Chen S; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Wilson JR; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Gamblin SJ; Constellation Pharmaceuticals, Inc., 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
J Med Chem ; 59(21): 9928-9941, 2016 11 10.
Article de En | MEDLINE | ID: mdl-27739677
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Texte intégral: 1 Collection: 01-internacional Base de données: MEDLINE Sujet principal: Pipéridines / Lymphome B / Histone-lysine N-methyltransferase / Essais cliniques de phase I comme sujet / Antienzymes / Indoles / Antinéoplasiques Type d'étude: Diagnostic_studies Limites: Animals / Humans Langue: En Journal: J Med Chem Sujet du journal: QUIMICA Année: 2016 Type de document: Article Pays d'affiliation: États-Unis d'Amérique
Texte intégral
Ajouter à My VHL
Imprimer
XML
PubMed Links
Recherche sur Google

Texte intégral: 1 Collection: 01-internacional Base de données: MEDLINE Sujet principal: Pipéridines / Lymphome B / Histone-lysine N-methyltransferase / Essais cliniques de phase I comme sujet / Antienzymes / Indoles / Antinéoplasiques Type d'étude: Diagnostic_studies Limites: Animals / Humans Langue: En Journal: J Med Chem Sujet du journal: QUIMICA Année: 2016 Type de document: Article Pays d'affiliation: États-Unis d'Amérique