Thiol-based SAHA analogues as potent histone deacetylase inhibitors
…, A Kouketsu, A Matsuura, A Kohara, S Ninomiya…
Index: Suzuki, Takayoshi; Kouketsu, Akiyasu; Matsuura, Azusa; Kohara, Arihiro; Ninomiya, Shin-Ichi; Kohda, Kohfuku; Miyata, Naoki Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 12 p. 3313 - 3317
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Citation Number: 86
Abstract
In order to find novel nonhydroxamate histone deacetylase (HDAC) inhibitors, a series of thiol-based compounds modeled after suberoylanilide hydroxamic acid (SAHA) was synthesized, and their inhibitory effect on HDACs was evaluated. Compound 6, in which the hydroxamic acid of SAHA was replaced by a thiol, was found to be as potent as SAHA, and optimization of this series led to the identification of HDAC inhibitors more potent than ...
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