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

Jiyong Lee; Joong Sup Shim; Sun Ah Jung; Seung Taek Lee; Ho Jeong Kwon

doi:10.1016/j.bmcl.2004.10.010

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

Jiyong Lee, Joong Sup Shim, Sun Ah Jung, Seung Taek Lee, Ho Jeong Kwon

Research output: Contribution to journal › Article › peer-review

18 Citations (Scopus)

Abstract

The discovery of a structurally new inhibitor of aminopeptidase N and its anti-angiogenic activity are reported. 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 μM. It also inhibited the basic fibroblast growth-factor-induced invasion of bovine aortic endothelial cells at low micromolar concentrations.

Original language	English
Pages (from-to)	181-183
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	15
Issue number	1
DOIs	https://doi.org/10.1016/j.bmcl.2004.10.010
Publication status	Published - 2005 Jan 3

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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abstract = "The discovery of a structurally new inhibitor of aminopeptidase N and its anti-angiogenic activity are reported. 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 Ki value of 3.5 μM. It also inhibited the basic fibroblast growth-factor-induced invasion of bovine aortic endothelial cells at low micromolar concentrations.",

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AU - Shim, Joong Sup

AU - Jung, Sun Ah

AU - Lee, Seung Taek

AU - Kwon, Ho Jeong

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

Abstract

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