Abstract
A series of novel aminopeptidase N inhibitors with 2,5-pyrrolidinedione scaffold were chemically synthesized. Their preliminary biological activities in enzyme kinetics and cell assay in vitro and anti-metastasis profile in vivo were also evaluated. The results indicated that all the compounds displayed potent inhibitory activity against aminopeptidase N. Compound 8f inhibited aminopeptidase N activity with IC(50) value of 1.0μM and displayed better activity profile in vivo than that of bestatin.
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
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Evaluation Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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CD13 Antigens / antagonists & inhibitors*
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CD13 Antigens / metabolism
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Dose-Response Relationship, Drug
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Drug Design*
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Drug Screening Assays, Antitumor
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Humans
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Models, Molecular
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Molecular Structure
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Peptidomimetics / chemical synthesis
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Peptidomimetics / chemistry
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Peptidomimetics / pharmacology*
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Phenylalanine / analogs & derivatives*
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Phenylalanine / chemical synthesis
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Phenylalanine / chemistry
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Phenylalanine / pharmacology
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Protease Inhibitors / chemical synthesis
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Protease Inhibitors / chemistry
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Protease Inhibitors / pharmacology*
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Structure-Activity Relationship
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Succinimides / chemical synthesis
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Succinimides / chemistry
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Succinimides / pharmacology*
Substances
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2-amino-N-(1-(2-(hydroxyamino)-2-oxoethyl)-2,5-dioxopyrrolidin-3-yl)-3-phenylpropanamide
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Antineoplastic Agents
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Peptidomimetics
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Protease Inhibitors
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Succinimides
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Phenylalanine
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CD13 Antigens