Document Report Card

ID: ALA3259719

Journal: ACS Med Chem Lett

Title: Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2.

Authors: Nasveschuk CG, Gagnon A, Garapaty-Rao S, Balasubramanian S, Campbell R, Lee C, Zhao F, Bergeron L, Cummings R, Trojer P, Audia JE, Albrecht BK, Harmange JC.

Abstract: 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.

CiteXplore: 24900844

DOI: 10.1021/ml400494b