Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2.

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.

SUBMITTER: Nasveschuk CG 

PROVIDER: S-EPMC4027731 | biostudies-literature | 2014 Apr

REPOSITORIES: biostudies-literature