Abstract
The aminopeptidase N (APN/CD13), overexpressed in tumor cells, plays a critical role in angiogenesis. In this study, we report the synthesis and in vitro enzyme inhibition assay of 1,3,4-thiadiazole scaffold compounds. These new compounds have potent inhibitory activities toward APN with IC(50) values in the micromol rang.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Angiogenesis Inhibitors / chemical synthesis
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Binding Sites
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CD13 Antigens / antagonists & inhibitors*
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CD13 Antigens / chemistry
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Drug Screening Assays, Antitumor
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Escherichia coli / enzymology
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Molecular Structure
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Neoplasm Proteins / antagonists & inhibitors
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Protease Inhibitors / chemical synthesis
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Protein Binding
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Structure-Activity Relationship
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Thiadiazoles / chemical synthesis*
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Thiadiazoles / pharmacology*
Substances
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Angiogenesis Inhibitors
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Neoplasm Proteins
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Protease Inhibitors
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Thiadiazoles
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CD13 Antigens