Identification of a potent non-hydroxamate histone deacetylase inhibitor by mechanism-based drug design

In order to find novel non-hydroxamate histone deacetylase (HDAC) inhibitors, we synthesized several suberoylanilide hydroxamic acid (SAHA)-based compounds designed on the basis of the catalytic mechanism of HDACs. Among these compounds, mercaptoacetamide 5b was found to be as potent as SAHA. Kineti...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2005-01, Vol.15 (2), p.331-335
Hauptverfasser:	Suzuki, Takayoshi, Matsuura, Azusa, Kouketsu, Akiyasu, Nakagawa, Hidehiko, Miyata, Naoki
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetamides - chemistry Acetylation Binding Sites Biological and medical sciences Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Histone deacetylase inhibitor Histone Deacetylase Inhibitors Hydroxamic Acids - chemical synthesis Hydroxamic Acids - pharmacology Kinetics Medical sciences Miscellaneous Models, Molecular Non-hydroxamate Pharmacology. Drug treatments Structure-Activity Relationship Sulfhydryl Compounds - chemistry Zinc - chemistry
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