Design, synthesis and preliminary activity evaluation of novel L-lysine derivatives as aminopeptidase N/CD13 inhibitors.
A novel class of L-lysine derivatives as aminopeptidase N (APN) inhibitors was designed and synthesized. Activity evaluation showed that compound C7 (IC(50) = 9.6 +/-1.3 microM) and C20 (IC(50) = 13.6 +/- 1.9 microM) were equivalent to the positive control Bestatin (IC(50) = 11.3 +/- 1.6 microM).
Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong 250012, PR China.
Qiang
Q
Wang
Fuming
F
Xu
Jiajia
J
Mou
Jian
J
Zhang
Luqing
L
Shang
Yepeng
Y
Luan
Yumei
Y
Yuan
Yingzi
Y
Liu
Minyong
M
Li
Hao
H
Fang
Binghe
B
Wang
Wenfang
W
Xu
D000970:Antineoplastic Agents; D018826:CD13 Antigens / Q000037:antagonists & inhibitors*; D020134:Catalytic Domain; D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D007930:Leucine / Q000031:analogs & derivatives / Q000737:chemistry / Q000378:metabolism; D008239:Lysine / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism; D008958:Models, Molecular
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D018826:CD13 Antigens; D007930:Leucine; C012211:ubenimex; D008239:Lysine