Novel 3-phenylpropane-1,2-diamine derivates as inhibitors of aminopeptidase N (APN)

Bioorg Med Chem. 2008 Dec 1;16(23):9984-90. doi: 10.1016/j.bmc.2008.10.025. Epub 2008 Oct 14.

Abstract

Aminopeptidase N (APN) is an essential peptidase involved in the process of tumor invasion and metastasis. Here we describe a novel class of inhibitor with 3-phenylpropane-1,2-diamine as scaffold to APN. Preliminary activity evaluation with enzyme inhibition studies showed that compound 12i exhibited potent and selective inhibitory activity towards APN with the IC(50) value 15.5+/-1.2microM.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • CD13 Antigens / antagonists & inhibitors*
  • CD13 Antigens / chemistry
  • CD13 Antigens / pharmacology
  • Cells, Cultured
  • Diamines / chemical synthesis
  • Diamines / chemistry
  • Diamines / pharmacology*
  • HL-60 Cells
  • Humans
  • Inhibitory Concentration 50
  • Matrix Metalloproteinase 2 / pharmacology
  • Matrix Metalloproteinase Inhibitors
  • Microsomes / drug effects
  • Microsomes / metabolism
  • Protease Inhibitors / chemical synthesis
  • Protease Inhibitors / chemistry
  • Protease Inhibitors / pharmacology*
  • Structure-Activity Relationship

Substances

  • Diamines
  • Matrix Metalloproteinase Inhibitors
  • Protease Inhibitors
  • CD13 Antigens
  • Matrix Metalloproteinase 2