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

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 s...

Descripción completa

Detalles Bibliográficos
Autores principales: Mou, Jiajia, Fang, Hao, Jing, Fanbo, Wang, Qiang, Liu, Yingzi, Zhu, Huawei, Shang, Luqing, Wang, Xuejian, Xu, Wenfang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Ltd. 2009
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7125801/
https://www.ncbi.nlm.nih.gov/pubmed/19454370
http://dx.doi.org/10.1016/j.bmc.2009.04.056
Descripción
Sumario: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.

Ejemplares similares