N-hydroxy-2-(naphthalene-2-ylsulfanyl)-acetamide, a novel hydroxamic acid-based inhibitor of aminopeptidase N and its anti-angiogenic activity.
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.
Lee
Jiyong
J
Chemical Genomics National Research Laboratory, Department of Bioscience and Biotechnology, Institute of Bioscience, Sejong University, 98 Kunja-dong, Kwangjin-gu, Seoul 143-747, Korea.
Shim
Joong Sup
JS
Jung
Sun-Ah
SA
Lee
Seung-Taek
ST
Kwon
Ho Jeong
HJ
D000081:Acetamides / Q000494:pharmacology*; D020533:Angiogenesis Inhibitors / Q000494:pharmacology*; D000818:Animals; D001011:Aorta / Q000166:cytology / Q000187:drug effects; D018826:CD13 Antigens / Q000037:antagonists & inhibitors*; D002417:Cattle; D002478:Cells, Cultured; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D016222:Fibroblast Growth Factor 2 / Q000037:antagonists & inhibitors; D006877:Hydroxamic Acids / Q000737:chemistry*; D009281:Naphthalenes / Q000494:pharmacology*
D000081:Acetamides; D020533:Angiogenesis Inhibitors; D004791:Enzyme Inhibitors; D006877:Hydroxamic Acids; C500025:N-hydroxy-2-(naphthalene-2-ylsulfanyl)-acetamide; D009281:Naphthalenes; D016222:Fibroblast Growth Factor 2; D018826:CD13 Antigens