Alpha-keto amides as inhibitors of histone deacetylase

Bioorg Med Chem Lett. 2003 Oct 6;13(19):3331-5. doi: 10.1016/s0960-894x(03)00685-1.

Abstract

Alpha-keto ester and amides were found to be potent inhibitors of histone deacetylase. Nanomolar inhibitors against the isolated enzyme and sub-micromolar inhibitors of cellular proliferation were obtained. The alpha-keto amide 30 also exhibited significant anti-tumor effects in an in vivo tumor model.

MeSH terms

  • Amides / chemistry*
  • Amides / pharmacology*
  • Animals
  • Cell Line, Tumor
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology*
  • Histone Deacetylase Inhibitors*
  • Histone Deacetylases / metabolism
  • Humans
  • Mice
  • Xenograft Model Antitumor Assays / methods

Substances

  • Amides
  • Enzyme Inhibitors
  • Histone Deacetylase Inhibitors
  • Histone Deacetylases