Synthesis and Biological Evaluation of ortho‐Aryl N‐Hydroxycinnamides as Potent Histone Deacetylase (HDAC) 8 Isoform‐Selective Inhibitors

Abstract excerpt

Histone deacetylases (HDACs) are a family of enzymes that play a crucial role in biological process and diseases. In contrast to other isozymes, HDAC8 is uniquely incapable of histone acetylation. In order to delineate its physiological function, we developed HDAC8-selective inhibitors using knowledge-based design combined with structural modeling techniques. Enzyme inhibitory analysis demonstrated that some of...

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