Novel aminopeptidase N inhibitors derived from 1,3,4-thiadiazole scaffold.
The aminopeptidase N (APN/CD13), overexpressed in tumor cells, plays a critical role in angiogenesis. In this study, we report the synthesis and in vitro enzyme inhibition assay of 1,3,4-thiadiazole scaffold compounds. These new compounds have potent inhibitory activities toward APN with IC(50) values in the micromol rang.
Tu
GuoGang
G
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, ShanDong University, 44, West Culture Road, Ji'nan 250012, PR China.
Li
ShaoHua
S
Huang
HuiMing
H
Li
Gang
G
Xiong
Fang
F
Mai
Xi
X
Zhu
HuaWei
H
Kuang
BinHai
B
Xu
Wen Fang
WF
D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis; D001665:Binding Sites; D018826:CD13 Antigens / Q000037:antagonists & inhibitors* / Q000737:chemistry; D004354:Drug Screening Assays, Antitumor; D004926:Escherichia coli / Q000201:enzymology; D015394:Molecular Structure; D009363:Neoplasm Proteins / Q000037:antagonists & inhibitors; D011480:Protease Inhibitors / Q000138:chemical synthesis; D011485:Protein Binding; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
D020533:Angiogenesis Inhibitors; D009363:Neoplasm Proteins; D011480:Protease Inhibitors; D013830:Thiadiazoles; D018826:CD13 Antigens