1377995-67-9Relevant articles and documents
Discovery and optimization of tetramethylpiperidinyl benzamides as inhibitors of EZH2
Nasveschuk, Christopher G.,Gagnon, Alexandre,Garapaty-Rao, Shivani,Balasubramanian, Srividya,Campbell, Robert,Lee, Christina,Zhao, Feng,Bergeron, Louise,Cummings, Richard,Trojer, Patrick,Audia, James E.,Albrecht, Brian K.,Harmange, Jean-Christophe P.
supporting information, p. 378 - 383 (2014/05/06)
The identification and development of a novel series of small molecule Enhancer of Zeste Homologue 2 (EZH2) inhibitors is described. A concise and modular synthesis enabled the rapid development of structure-activity relationships, which led to the identification of 44 as a potent, SAM-competitive inhibitor of EZH2 that dose-dependently decreased global H3K27me3 in KARPAS-422 lymphoma cells.