Design and synthesis of non-hydroxamate histone deacetylase inhibitors: identification of a selective histone acetylating agent |
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| Authors: | Suzuki Takayoshi Matsuura Azusa Kouketsu Akiyasu Hisakawa Shinya Nakagawa Hidehiko Miyata Naoki |
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| Institution: | Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan. suzuki@phar.nagoya-cu.ac.jp |
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| 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 alpha-tubulin in HCT116 cells. |
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