title: Thiol-based SAHA analogues as potent histone deacetylase inhibitors.
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.
authors.affiliation: 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
authors.forename: Takayoshi
authors.initials: T
authors.lastname: Suzuki
authors.forename: Akiyasu
authors.initials: A
authors.lastname: Kouketsu
authors.forename: Azusa
authors.initials: A
authors.lastname: Matsuura
authors.forename: Arihiro
authors.initials: A
authors.lastname: Kohara
authors.forename: Shin-Ichi
authors.initials: S
authors.lastname: Ninomiya
authors.forename: Kohfuku
authors.initials: K
authors.lastname: Kohda
authors.forename: Naoki
authors.initials: N
authors.lastname: Miyata
mesh_terms: D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D056572:Histone Deacetylase Inhibitors; D006655:Histone Deacetylases / Q000378:metabolism; D006877:Hydroxamic Acids / Q000737:chemistry* / Q000494:pharmacology; D013438:Sulfhydryl Compounds / Q000737:chemistry* / Q000494:pharmacology; D000077337:Vorinostat
chemical_list: D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors; D006877:Hydroxamic Acids; D013438:Sulfhydryl Compounds; D000077337:Vorinostat; D006655:Histone Deacetylases