Novel CoA-polyamine conjugates for effective inhibition of spermine/spermidine-N1-acetyltransferase

Nucleosides Nucleotides Nucleic Acids. 2007;26(10-12):1245-8. doi: 10.1080/15257770701528214.

Abstract

New mimics of the transition state of spermine/spermidine-N(1)-acetyltransferase reaction were prepared starting from aminooxy analogues of spermidine or spermine and SH-CoA. The activity depended on the structure of polyamine fragment of the conjugate and best of the synthesized compounds were active at micromolar concentrations.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetyltransferases / antagonists & inhibitors*
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Coenzyme A / chemistry
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Molecular Mimicry
  • Spermidine / analogs & derivatives*
  • Spermine / analogs & derivatives*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Spermine
  • Acetyltransferases
  • diamine N-acetyltransferase
  • Coenzyme A
  • Spermidine