Trifluoromethyl ketones as inhibitors of histone deacetylase

Bioorg Med Chem Lett. 2002 Dec 2;12(23):3443-7. doi: 10.1016/s0960-894x(02)00754-0.

Abstract

Trifluoromethyl ketones were found to be inhibitors of histone deacetylases (HDACs). Optimization of this series led to the identification of submicromolar inhibitors such as 20 that demonstrated antiproliferative effects against the HT1080 and MDA 435 cell lines.

MeSH terms

  • Acetylation
  • Blotting, Western
  • Breast Neoplasms / metabolism
  • Cell Cycle / drug effects
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology*
  • Fibrosarcoma / metabolism
  • Histone Deacetylase Inhibitors*
  • Histones / metabolism
  • Humans
  • Hydrocarbons, Fluorinated / chemistry
  • Hydrocarbons, Fluorinated / pharmacology
  • Ketones / chemistry*
  • Ketones / pharmacology*
  • Structure-Activity Relationship
  • Tumor Cells, Cultured

Substances

  • Enzyme Inhibitors
  • Histone Deacetylase Inhibitors
  • Histones
  • Hydrocarbons, Fluorinated
  • Ketones