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

Kanghui Yang, Jinghong Fen, Hao Fang, Lei Zhang, Jianzhi Gong, Wenfang Xu

Index: J. Enzyme Inhib. Med. Chem. 27(2) , 302-10, (2012)

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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.