Design, synthesis and preliminary activity evaluation of novel L-lysine derivatives as aminopeptidase N/CD13 inhibitors

Protein Pept Lett. 2010 Jul;17(7):847-53. doi: 10.2174/092986610791306661.

Abstract

A novel class of L-lysine derivatives as aminopeptidase N (APN) inhibitors was designed and synthesized. Activity evaluation showed that compound C7 (IC(50) = 9.6 +/-1.3 microM) and C20 (IC(50) = 13.6 +/- 1.9 microM) were equivalent to the positive control Bestatin (IC(50) = 11.3 +/- 1.6 microM).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents
  • CD13 Antigens / antagonists & inhibitors*
  • Catalytic Domain
  • Cell Line, Tumor
  • Enzyme Inhibitors* / chemistry
  • Enzyme Inhibitors* / metabolism
  • Humans
  • Leucine / analogs & derivatives
  • Leucine / chemistry
  • Leucine / metabolism
  • Lysine* / analogs & derivatives
  • Lysine* / chemical synthesis
  • Lysine* / chemistry
  • Lysine* / metabolism
  • Models, Molecular

Substances

  • Antineoplastic Agents
  • Enzyme Inhibitors
  • CD13 Antigens
  • Leucine
  • ubenimex
  • Lysine