Abstract
A series of novel 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives were designed, synthesized and assayed for their activities against aminopeptidase N (APN/CD13) and MMP-2. The results showed that most compounds exhibited higher inhibitory activities against APN than that of MMP-2. Within this series, compound 12h (IC(50)=6.28 ± 0.11 μM) showed similar inhibitory activities compared with Bestatin (IC(50)=5.55 ± 0.01 μM), and it could be used as novel lead compound for the future APN inhibitors development as anticancer agents.
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
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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 / pharmacology
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CD13 Antigens / antagonists & inhibitors*
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CD13 Antigens / chemistry
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CD13 Antigens / metabolism
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Drug Design
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Humans
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Protease Inhibitors / chemical synthesis*
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Protease Inhibitors / pharmacology
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Structure-Activity Relationship
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Tetrahydroisoquinolines / chemical synthesis*
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Tetrahydroisoquinolines / chemistry
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Tetrahydroisoquinolines / pharmacology*
Substances
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Antineoplastic Agents
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Protease Inhibitors
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Tetrahydroisoquinolines
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1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
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CD13 Antigens