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 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.
Mou
Jiajia
J
Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong, PR China.
Fang
Hao
H
Jing
Fanbo
F
Wang
Qiang
Q
Liu
Yingzi
Y
Zhu
Huawei
H
Shang
Luqing
L
Wang
Xuejian
X
Xu
Wenfang
W
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001120:Arginine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D018826:CD13 Antigens / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D006801:Humans; D020778:Matrix Metalloproteinase 2 / Q000378:metabolism; D061965:Matrix Metalloproteinase Inhibitors; D008862:Microsomes, Liver / Q000201:enzymology; D008958:Models, Molecular; D015394:Molecular Structure; D011485:Protein Binding; D013329:Structure-Activity Relationship; D013552:Swine
D000970:Antineoplastic Agents; D061965:Matrix Metalloproteinase Inhibitors; D001120:Arginine; D018826:CD13 Antigens; D020778:Matrix Metalloproteinase 2