N-hydroxy-2-(naphthalene-2-ylsulfanyl)-acetamide, a novel hydroxamic acid-based inhibitor of aminopeptidase N and its anti-angiogenic activity

  • Bioorg Med Chem Lett. 2005 Jan 3;15(1):181-3. doi: 10.1016/j.bmcl.2004.10.010.
Jiyong Lee  1 ,  Joong Sup Shim ,  Sun-Ah Jung ,  Seung-Taek Lee ,  Ho Jeong Kwon
Affiliations
  • 1. Chemical Genomics National Research Laboratory, Department of Bioscience and Biotechnology, Institute of Bioscience, Sejong University, 98 Kunja-dong, Kwangjin-gu, Seoul 143-747, Korea.
PMID: 15582436 DOI: 10.1016/j.bmcl.2004.10.010
Abstract

In the course of our screening, N-hydroxy-2-(naphthalene-2-ylsulfanyl)-acetamide (1), which contains a metal-chelating hydroxamate group, has been identified as a potent inhibitor of Aminopeptidase N (APN, EC 3.4.11.2). Compound 1 potently inhibited APN activity with a K(i) value of 3.5 microM. It also inhibited the basic fibroblast growth-factor-induced invasion of bovine aortic endothelial cells at low micromolar concentrations.