title: Novel aminopeptidase N (APN/CD13) inhibitors derived from chloramphenicol amine.
abstract: Aminopeptidase N (APN) is involved in different physiological and pathological processes of tumor cells, including proliferation, invasion, apoptosis and metastasis. Herein one series of compounds derived from commercially available (1S,2S)-2-amino-1-(4-nitrophenyl) propane-1,3-diol have been designed and synthesized. Furthermore, preliminary activity evaluation showed that some compounds elicited moderate inhibitory activity against APN with compounds 10e (IC(50)=6.1±0.5 μM) possessing the best efficacy, which could be used as the lead compound in the future for anticancer agents research.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong, PR China.
authors.forename: Meirong
authors.initials: M
authors.lastname: Jia
authors.forename: Kanghui
authors.initials: K
authors.lastname: Yang
authors.forename: Hao
authors.initials: H
authors.lastname: Fang
authors.forename: Yingying
authors.initials: Y
authors.lastname: Xu
authors.forename: Siwei
authors.initials: S
authors.lastname: Sun
authors.forename: Li
authors.initials: L
authors.lastname: Su
authors.forename: Wenfang
authors.initials: W
authors.lastname: Xu
mesh_terms: D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D001665:Binding Sites; D018826:CD13 Antigens / Q000037:antagonists & inhibitors* / Q000378:metabolism; D002701:Chloramphenicol / Q000737:chemistry*; D003198:Computer Simulation; D004151:Dipeptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D004354:Drug Screening Assays, Antitumor; D011412:Propanolamines / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D013329:Structure-Activity Relationship
chemical_list: C568685:2-amino-N-(1-(2-amino-3-(4-aminophenyl)-3-hydroxypropylamino)-1-oxo-3-phenylpropan-2-yl)-4-methylpentanamide; D000588:Amines; D000970:Antineoplastic Agents; D004151:Dipeptides; D011412:Propanolamines; D011480:Protease Inhibitors; D002701:Chloramphenicol; D018826:CD13 Antigens