Abstract
A series of novel l-lysine derivatives were designed, synthesized, and assayed for their inhibitory activities on amino-peptidase N (APN)/CD13 and matrix metalloproteinase-2 (MMP-2). The preliminary biological test showed that most of the compounds displayed a high inhibitory activity against MMP-2 and a low activity against APN except compound B6 which exhibited good potency (IC(50)=13.2microM) similar with APN inhibitor Bestatin (IC(50)=15.5microM), and could be used as lead compound in the future.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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CD13 Antigens / antagonists & inhibitors*
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Crystallography, X-Ray
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Drug Design*
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Drug Evaluation, Preclinical
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Inhibitory Concentration 50
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Leucine / analogs & derivatives
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Leucine / pharmacology
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Lysine / analogs & derivatives
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Lysine / chemical synthesis
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Lysine / pharmacology*
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Matrix Metalloproteinase Inhibitors
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Models, Molecular
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Molecular Structure
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Quantitative Structure-Activity Relationship*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Matrix Metalloproteinase Inhibitors
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CD13 Antigens
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Leucine
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ubenimex
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Lysine