doi: 10.1016/j.bmcl.2004.03.063.
Thiol-based SAHA analogues as potent histone deacetylase inhibitors
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- PMID: 15149697
- DOI: 10.1016/j.bmcl.2004.03.063
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Thiol-based SAHA analogues as potent histone deacetylase inhibitors
Bioorg Med Chem Lett.
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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 SAHA.
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