Design and synthesis of non-hydroxamate histone deacetylase inhibitors: identification of a selective histone acetylating agent

A series of suberoylanilide hydroxamic acid (SAHA)-based non-hydroxamates was designed, synthesized, and evaluated for their histone deacetylase (HDAC) inhibitory activity. Among these, methyl sulfoxide 15 inhibited HDACs in enzyme assays and caused hyperacetylation of histone H4 while not inducing the accumulation of acetylated α-tubulin in HCT116 cells.

A series of non-hydroxamate compounds was designed, and synthesized as histone deacetylase (HDAC) inhibitors. In this series, compound 15 inhibited HDACs in vitro and caused the accumulation of acetylated histone H4 without inducing the accumulation of acetylated α-tubulin in HCT116 cells.Figure optionsDownload as PowerPoint slide