Design and synthesis of novel hybrid benzamide-peptide histone deacetylase inhibitors

Bioorg Med Chem Lett. 2009 Jul 15;19(14):3928-31. doi: 10.1016/j.bmcl.2009.03.085. Epub 2009 Mar 25.

Abstract

We designed and synthesized a series of novel hybrid histone deacetylase inhibitors based on conjugation of benzamide-type inhibitors with either linear or cyclic peptides. Linear tetrapeptides (compounds 13 and 14), cyclic tetrapeptides (compounds 1 and 11), and heptanediamide-peptide conjugates (compounds 10, 12, 15 and 16) were synthesized through on-resin solid-phase peptide synthesis (SPPS). All compounds were found to be moderate HDAC1 and HDAC3 inhibitors, with IC(50) values ranging from 1.3 microM to 532 microM. Interestingly, compound 15 showed 19-fold selectivity for HDAC3 versus HDAC1.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzamides / chemistry*
  • Cyclization
  • Drug Design
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • Histone Deacetylase 1
  • Histone Deacetylase Inhibitors*
  • Histone Deacetylases / metabolism
  • Humans
  • Neuroprotective Agents / chemical synthesis*
  • Neuroprotective Agents / chemistry
  • Neuroprotective Agents / pharmacology
  • Peptides / chemical synthesis
  • Peptides / chemistry*

Substances

  • Benzamides
  • Enzyme Inhibitors
  • Histone Deacetylase Inhibitors
  • Neuroprotective Agents
  • Peptides
  • benzamide
  • HDAC1 protein, human
  • Histone Deacetylase 1
  • Histone Deacetylases
  • histone deacetylase 3