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.


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


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