Discovery of pyrimidyl-5-hydroxamic acids as new potent histone deacetylase inhibitors

Eur J Med Chem. 2005 Jun;40(6):597-606. doi: 10.1016/j.ejmech.2005.01.008. Epub 2005 Mar 3.

Abstract

A series of pyrimidyl-5-hydroxamic acids was prepared for evaluation as inhibitors of histone deacetylase (HDAC). Amino-2-pyrimidinyl can be used as a linker to provide HDAC inhibitors of good enzymatic potency.

MeSH terms

  • Cell Proliferation / drug effects
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • Female
  • HeLa Cells
  • Histone Deacetylase Inhibitors*
  • Humans
  • Hydroxamic Acids / chemical synthesis*
  • Hydroxamic Acids / chemistry
  • Hydroxamic Acids / pharmacology*
  • Inhibitory Concentration 50
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacology*
  • Spectrometry, Mass, Electrospray Ionization

Substances

  • Enzyme Inhibitors
  • Histone Deacetylase Inhibitors
  • Hydroxamic Acids
  • Pyrimidines