title: Novel 3-phenylpropane-1,2-diamine derivates as inhibitors of aminopeptidase N (APN).
abstract: 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.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Shandong University, 44 West Culture Road, 250012 Ji'nan, Shandong, PR China.
authors.forename: Luqing
authors.initials: L
authors.lastname: Shang
authors.forename: Qiang
authors.initials: Q
authors.lastname: Wang
authors.forename: Hao
authors.initials: H
authors.lastname: Fang
authors.forename: Jiajia
authors.initials: J
authors.lastname: Mu
authors.forename: Xuejian
authors.initials: X
authors.lastname: Wang
authors.forename: Yumei
authors.initials: Y
authors.lastname: Yuan
authors.forename: Binghe
authors.initials: B
authors.lastname: Wang
authors.forename: Wenfang
authors.initials: W
authors.lastname: Xu
mesh_terms: 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
chemical_list: D003959:Diamines; D061965:Matrix Metalloproteinase Inhibitors; D011480:Protease Inhibitors; D018826:CD13 Antigens; D020778:Matrix Metalloproteinase 2