Pyrazole-based inhibitors of enhancer of zeste homologue 2 induce apoptosis and autophagy in cancer cells

Novel pyrazole-based EZH2 inhibitors have been prepared through a molecular pruning approach from known inhibitors bearing a bicyclic moiety as a central scaffold. The hit compound 1o (N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-methyl-1-phenyl-1H-pyrazole-4-carboxamide) showed low micr...

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Veröffentlicht in:	Philosophical transactions of the Royal Society of London. Series B. Biological sciences 2018-06, Vol.373 (1748), p.20170150-20170150
Hauptverfasser:	Mellini, Paolo, Marrocco, Biagina, Borovika, Diana, Polletta, Lucia, Carnevale, Ilaria, Saladini, Serena, Stazi, Giulia, Zwergel, Clemens, Trapencieris, Peteris, Ferretti, Elisabetta, Tafani, Marco, Valente, Sergio, Mai, Antonello
Format:	Artikel
Sprache:	eng
Schlagworte:	Apoptosis Autophagy Cancer Enhancer Of Zeste Homologue 2 Inhibitors Epigenetics Homology Inhibitors Leukemia Neuroblastoma Phagocytosis Pruning Pyrazole
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