Synthesis of a novel series of L-isoserine derivatives as aminopeptidase N inhibitors

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 mu M) compared with the positive control bestatin (half maximal inhibitory concentration (IC50) of 7.3 mu M), but also had a potent antiproliferative activity against human cancer cell lines cells.