Novel 3-phenylpropane-1,2-diamine derivates as inhibitors of aminopeptidase N (APN).
Aminopeptidase N (APN) is an essential peptidase involved in the process of tumor invasion and metastasis. Here we describe a novel class of inhibitor with 3-phenylpropane-1,2-diamine as scaffold to APN. Preliminary activity evaluation with enzyme inhibition studies showed that compound 12i exhibited potent and selective inhibitory activity towards APN with the IC(50) value 15.5+/-1.2microM.
Shang
Luqing
L
Department of Medicinal Chemistry, School of Pharmacy, Shandong University, 44 West Culture Road, 250012 Ji'nan, Shandong, PR China.
Wang
Qiang
Q
Fang
Hao
H
Mu
Jiajia
J
Wang
Xuejian
X
Yuan
Yumei
Y
Wang
Binghe
B
Xu
Wenfang
W
D018826:CD13 Antigens / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000494:pharmacology; D002478:Cells, Cultured; D003959:Diamines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D018922:HL-60 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D020778:Matrix Metalloproteinase 2 / Q000494:pharmacology; D061965:Matrix Metalloproteinase Inhibitors; D008861:Microsomes / Q000187:drug effects / Q000378:metabolism; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D003959:Diamines; D061965:Matrix Metalloproteinase Inhibitors; D011480:Protease Inhibitors; D018826:CD13 Antigens; D020778:Matrix Metalloproteinase 2