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).
Wang
Qiang
Q
Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong 250012, PR China.
Xu
Fuming
F
Mou
Jiajia
J
Zhang
Jian
J
Shang
Luqing
L
Luan
Yepeng
Y
Yuan
Yumei
Y
Liu
Yingzi
Y
Li
Minyong
M
Fang
Hao
H
Wang
Binghe
B
Xu
Wenfang
W
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