ACS medicinal chemistry letters · 2018
Improved Selective Class I HDAC and Novel Selective HDAC3 Inhibitors: Beyond Hydroxamic Acids and Benzamides.
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Bresciani Alberto, Ontoria Jesus M, Biancofiore Ilaria, Cellucci Antonella, Ciammaichella Alina, Di Marco Annalise, Ferrigno Federica, Francone Alessandra, Malancona Savina, Monteagudo Edith, Nizi Emanuela, Pace Paola, Ponzi Simona, Rossetti Ilaria, Veneziano Maria, Summa Vincenzo, Harper Steven
Аннотация
The application of class I HDAC inhibitors as cancer therapies is well established, but more recently their development for nononcological indications has increased. We report here on the generation of improved class I selective human HDAC inhibitors based on an ethylketone zinc binding group (ZBG) in place of the hydroxamic acid that features the majority of HDAC inhibitors. We also describe a novel set of HDAC3 isoform selective inhibitors that show stronger potency and selectivity than the most commonly used HDAC3 selective tool compound RGFP966. These compounds are again based on an alternative ZBG with respect to the ortho-anilide that is featured in HDAC3 selective compounds reported to date.