title: Novel leucine ureido derivatives as inhibitors of aminopeptidase N (APN).
abstract: Aminopeptidase N (APN/CD13) over expressed on tumor cells, plays a critical role in tumor invasion, metastasis, and tumor angiogenesis. Here we described the design, synthesis and preliminary activity studies of novel leucine ureido derivatives as aminopeptidase N (APN/CD13) inhibitors. The results showed that compound 8c had the most potent inhibitory activity against APN with the IC50 value to 0.06 ± 0.041 μM, which could be used for further anticancer agent research.
authors: Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University 44, West Culture Road, Jinan 250012, PR China.
authors: Chunhua
authors: C
authors: Ma
authors: Kang
authors: K
authors: Jin
authors: Jiangying
authors: J
authors: Cao
authors: Lei
authors: L
authors: Zhang
authors: Xiaoguang
authors: X
authors: Li
authors: Wenfang
authors: W
authors: Xu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D018826:CD13 Antigens / Q000037:antagonists & inhibitors* / Q000378:metabolism; D045744:Cell Line, Tumor; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D007930:Leucine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D062105:Molecular Docking Simulation; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology*; D011480:Protease Inhibitors / Q000737:chemistry / Q000494:pharmacology; D013552:Swine
chemical_list: D000970:Antineoplastic Agents; D011480:Protease Inhibitors; D018826:CD13 Antigens; D007930:Leucine