Design, synthesis and biological evaluation of novel l-lysine ureido derivatives as aminopeptidase N inhibitors

As the exopeptidase over-expressed in the cell surface of endothelial cells, aminopeptidase N (APN/CD13) is an essential target for tumor angiogenesis and metastasis. Based on the previous work of l-lysine amide derivatives in our laboratory, we designed and synthesized two series of l-lysine ureido derivatives as APN inhibitors. Within these compounds, one compound, 5d (IC50 = 4.51 μM), showed similar inhibitory effect compared with Bestatin (IC50 = 5.87 μM).

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