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.
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, ShanDong University, 44, West Culture Road, Ji'nan 250012, PR China.
GuoGang
G
Tu
ShaoHua
S
Li
HuiMing
H
Huang
Gang
G
Li
Fang
F
Xiong
Xi
X
Mai
HuaWei
H
Zhu
BinHai
B
Kuang
Wen Fang
WF
Xu
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