Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2.
نویسندگان
چکیده
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.
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ورودعنوان ژورنال:
- ACS medicinal chemistry letters
دوره 5 4 شماره
صفحات -
تاریخ انتشار 2014