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

Research paper by Jiajia J Mou, Hao H Fang, Fanbo F Jing, Qiang Q Wang, Yingzi Y Liu, Huawei H Zhu, Luqing L Shang, Xuejian X Wang, Wenfang W Xu

Indexed on: 21 May '09Published on: 21 May '09Published in: Bioorganic & Medicinal Chemistry


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 microM) showed similar inhibitory activities compared with bestatin (IC(50)=3.8 microM), which could be used as novel lead compounds for the future APN inhibitors development as anticancer agents.