Abstract
A series of novel L-isoserine derivatives were synthesised and evaluated for their ability to inhibit aminopeptidase N (APN)/CD13. In our preliminary biological results, some of these compounds possessed a potent inhibitory activity against the APN. Within this series, compound 14b not only showed similar enzyme inhibition (IC₅₀ of 12.2 μM) compared with the positive control bestatin (half maximal inhibitory concentration (IC₅₀) of 7.3 μM), but also had a potent antiproliferative activity against human cancer cell lines cells.
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 / metabolism
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Cell Proliferation / drug effects*
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Humans
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Leucine / analogs & derivatives
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Leucine / pharmacology
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Models, Molecular
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Neoplasms / drug therapy
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Protease Inhibitors / chemical synthesis*
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Protease Inhibitors / pharmacology
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Serine / analogs & derivatives*
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Serine / chemistry
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Structure-Activity Relationship
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents
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Protease Inhibitors
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Serine
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isoserine
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CD13 Antigens
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Leucine
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ubenimex