title: Synthesis of a novel series of L-isoserine derivatives as aminopeptidase N inhibitors.
abstract: A series of novel L-isoserine derivatives were synthesised and evaluated for their ability to inhibit aminopeptidase N (APN)/CD13. In our preliminary biological results, some of these compounds possessed a potent inhibitory activity against the APN. Within this series, compound 14b not only showed similar enzyme inhibition (IC₅₀ of 12.2 μM) compared with the positive control bestatin (half maximal inhibitory concentration (IC₅₀) of 7.3 μM), but also had a potent antiproliferative activity against human cancer cell lines cells.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Shan Dong University, 44 West Culture Road, Ji'nan, P R China.
authors.forename: Kanghui
authors.initials: K
authors.lastname: Yang
authors.forename: Jinghong
authors.initials: J
authors.lastname: Fen
authors.forename: Hao
authors.initials: H
authors.lastname: Fang
authors.forename: Lei
authors.initials: L
authors.lastname: Zhang
authors.forename: Jianzhi
authors.initials: J
authors.lastname: Gong
authors.forename: Wenfang
authors.initials: W
authors.lastname: Xu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D018826:CD13 Antigens / Q000037:antagonists & inhibitors* / Q000378:metabolism; D049109:Cell Proliferation / Q000187:drug effects*; D006801:Humans; D007930:Leucine / Q000031:analogs & derivatives / Q000494:pharmacology; D008958:Models, Molecular; D009369:Neoplasms / Q000188:drug therapy; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D012694:Serine / Q000031:analogs & derivatives* / Q000737:chemistry; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D011480:Protease Inhibitors; D012694:Serine; C072421:isoserine; D018826:CD13 Antigens; D007930:Leucine; C012211:ubenimex