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

T Suzuki, A Matsuura, A Kouketsu, S Hisakawa…

Index: Suzuki, Takayoshi; Matsuura, Azusa; Kouketsu, Akiyasu; Hisakawa, Shinya; Nakagawa, Hidehiko; Miyata, Naoki Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 13 p. 4332 - 4342

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Citation Number: 31

Abstract

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.