Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2

[Image: see text] 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,...

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Autors principals: 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.
Format: Artigo
Idioma:Inglês
Publicat: American Chemical Society 2014
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC4027731/
https://ncbi.nlm.nih.gov/pubmed/24900844
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml400494b
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