Thiol-based SAHA analogues as potent histone deacetylase inhibitors

Takayoshi Suzuki; Akiyasu Kouketsu; Azusa Matsuura; Arihiro Kohara; Shin-Ichi Ninomiya; Kohfuku Kohda; Naoki Miyata

doi:10.1016/j.bmcl.2004.03.063

Thiol-based SAHA analogues as potent histone deacetylase inhibitors

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3313-7. doi: 10.1016/j.bmcl.2004.03.063.

Authors

Takayoshi Suzuki¹, Akiyasu Kouketsu, Azusa Matsuura, Arihiro Kohara, Shin-Ichi Ninomiya, Kohfuku Kohda, Naoki Miyata

Affiliation

¹ Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Aichi, Nagoya 467-8603, Japan. suzuki@phar.nagoya-cu.ac.jp

PMID: 15149697
DOI: 10.1016/j.bmcl.2004.03.063

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / pharmacology
Histone Deacetylase Inhibitors*
Histone Deacetylases / metabolism
Hydroxamic Acids / chemistry*
Hydroxamic Acids / pharmacology
Sulfhydryl Compounds / chemistry*
Sulfhydryl Compounds / pharmacology
Vorinostat

Substances

Enzyme Inhibitors
Histone Deacetylase Inhibitors
Hydroxamic Acids
Sulfhydryl Compounds
Vorinostat
Histone Deacetylases