Novel aminopeptidase N inhibitors derived from 1,3,4-thiadiazole scaffold

Bioorg Med Chem. 2008 Jul 15;16(14):6663-8. doi: 10.1016/j.bmc.2008.05.081. Epub 2008 Jun 5.

Abstract

The aminopeptidase N (APN/CD13), overexpressed in tumor cells, plays a critical role in angiogenesis. In this study, we report the synthesis and in vitro enzyme inhibition assay of 1,3,4-thiadiazole scaffold compounds. These new compounds have potent inhibitory activities toward APN with IC(50) values in the micromol rang.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiogenesis Inhibitors / chemical synthesis
  • Binding Sites
  • CD13 Antigens / antagonists & inhibitors*
  • CD13 Antigens / chemistry
  • Drug Screening Assays, Antitumor
  • Escherichia coli / enzymology
  • Molecular Structure
  • Neoplasm Proteins / antagonists & inhibitors
  • Protease Inhibitors / chemical synthesis
  • Protein Binding
  • Structure-Activity Relationship
  • Thiadiazoles / chemical synthesis*
  • Thiadiazoles / pharmacology*

Substances

  • Angiogenesis Inhibitors
  • Neoplasm Proteins
  • Protease Inhibitors
  • Thiadiazoles
  • CD13 Antigens