860033-84-7Relevant academic research and scientific papers
Design, synthesis and primary activity evaluation of l-arginine derivatives as amino-peptidase N/CD13 inhibitors
Mou, Jiajia,Fang, Hao,Jing, Fanbo,Wang, Qiang,Liu, Yingzi,Zhu, Huawei,Shang, Luqing,Wang, Xuejian,Xu, Wenfang
experimental part, p. 4666 - 4673 (2009/12/01)
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 (IC50 = 5.3 and 5.1 μM) showed similar inhibitory activities compared with bestatin (IC50 = 3.8 μM), which could be used as novel lead compounds for the future APN inhibitors development as anticancer agents.
Design, synthesis, and evaluation of proline based melanocortin receptor ligands
Tian, Xinrong,Field, Timothy,Mazur, Adam W.,Ebetino, Frank H.,Wos, John A.,Crossdoersen, Doreen,Pinney, Beth B.,Sheldon, Russell J.
, p. 2819 - 2823 (2007/10/03)
A series of proline based melanocortin ligands has been developed on the basis of initial piperazine leads by using a more conformationally rigid scaffold. A number of these novel ligands showed significant binding affinity for MC3 and MC4 receptors.
