Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells

Since the histone modifying enzymes EZH2 and HDACs control a number of epigenetic-dependent carcinogenic pathways, we designed the first-in-class dual EZH2/HDAC inhibitor 5 displaying (sub)­micromolar inhibition against both targets. When tested in several cancer cell lines, the hybrid 5 impaired ce...

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Veröffentlicht in:	ACS medicinal chemistry letters 2020-05, Vol.11 (5), p.977-983
Hauptverfasser:	Romanelli, Annalisa, Stazi, Giulia, Fioravanti, Rossella, Zwergel, Clemens, Di Bello, Elisabetta, Pomella, Silvia, Perrone, Clara, Battistelli, Cecilia, Strippoli, Raffaele, Tripodi, Marco, del Bufalo, Donatella, Rota, Rossella, Trisciuoglio, Daniela, Mai, Antonello, Valente, Sergio
Format:	Artikel
Sprache:	eng
Schlagworte:	Letter
Online-Zugang:	Volltext
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