Design, synthesis, and QSAR studies of novel lysine derives as amino-peptidase N/CD13 inhibitors.
A series of novel l-lysine derivatives were designed, synthesized, and assayed for their inhibitory activities on amino-peptidase N (APN)/CD13 and matrix metalloproteinase-2 (MMP-2). The preliminary biological test showed that most of the compounds displayed a high inhibitory activity against MMP-2 and a low activity against APN except compound B6 which exhibited good potency (IC(50)=13.2microM) similar with APN inhibitor Bestatin (IC(50)=15.5microM), and could be used as lead compound in the future.
Wang
Qiang
Q
Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong 250012, PR China.
Chen
Maoying
M
Zhu
Huawei
H
Zhang
Jie
J
Fang
Hao
H
Wang
Binghe
B
Xu
Wenfang
W
D018826:CD13 Antigens / Q000037:antagonists & inhibitors*; D018360:Crystallography, X-Ray; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D020128:Inhibitory Concentration 50; D007930:Leucine / Q000031:analogs & derivatives / Q000494:pharmacology; D008239:Lysine / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D061965:Matrix Metalloproteinase Inhibitors; D008958:Models, Molecular; D015394:Molecular Structure; D021281:Quantitative Structure-Activity Relationship; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D061965:Matrix Metalloproteinase Inhibitors; D018826:CD13 Antigens; D007930:Leucine; C012211:ubenimex; D008239:Lysine