Design, synthesis and primary activity evaluation of l-arginine derivatives as amino-peptidase N/CD13 inhibitors

Abstract A series of l -arginine derivatives were designed, synthesized and assayed for their activities against amino-peptidase N (APN)/CD13 and metalloproteinase-2 (MMP-2). The results showed that most compounds exhibited high inhibitory activities against APN and low activities against MMP-2. Within this series, two compounds 5q and 5s (IC 50  = 5.3 and 5.1 μM) showed similar inhibitory activities compared with bestatin (IC 50  = 3.8 μM), which could be used as novel lead compounds for the future APN inhibitors development as anticancer agents.