Abstract
Aminopeptidase N (APN) is involved in different physiological and pathological processes of tumor cells, including proliferation, invasion, apoptosis and metastasis. Herein one series of compounds derived from commercially available (1S,2S)-2-amino-1-(4-nitrophenyl) propane-1,3-diol have been designed and synthesized. Furthermore, preliminary activity evaluation showed that some compounds elicited moderate inhibitory activity against APN with compounds 10e (IC(50)=6.1±0.5 μM) possessing the best efficacy, which could be used as the lead compound in the future for anticancer agents research.
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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Amines / chemical synthesis
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Amines / chemistry*
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Amines / toxicity
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / toxicity
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Binding Sites
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CD13 Antigens / antagonists & inhibitors*
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CD13 Antigens / metabolism
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Chloramphenicol / chemistry*
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Computer Simulation
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Dipeptides / chemical synthesis
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Dipeptides / chemistry*
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Dipeptides / toxicity
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Drug Screening Assays, Antitumor
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Propanolamines / chemical synthesis
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Propanolamines / chemistry*
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Propanolamines / toxicity
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Protease Inhibitors / chemical synthesis
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Protease Inhibitors / chemistry*
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Protease Inhibitors / toxicity
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Structure-Activity Relationship
Substances
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2-amino-N-(1-(2-amino-3-(4-aminophenyl)-3-hydroxypropylamino)-1-oxo-3-phenylpropan-2-yl)-4-methylpentanamide
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Amines
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Antineoplastic Agents
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Dipeptides
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Propanolamines
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Protease Inhibitors
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Chloramphenicol
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CD13 Antigens