2. Academic Validation
  3. Novel leucine ureido derivatives as aminopeptidase N inhibitors. Design, synthesis and activity evaluation

Novel leucine ureido derivatives as aminopeptidase N inhibitors. Design, synthesis and activity evaluation

  • Eur J Med Chem. 2016 Jan 27:108:21-27. doi: 10.1016/j.ejmech.2015.11.021.
Chunhua Ma 1,  Jiangying Cao 2,  Xuewu Liang 2,  Yongxue Huang 2,  Ping Wu 3,  Yingxia Li 3,  Wenfang Xu 2,  Yingjie Zhang 4
Affiliations

Affiliations

  • 1 School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China; School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.
  • 2 School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.
  • 3 School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China.
  • 4 School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China. Electronic address: zhangyingjie@sdu.edu.cn.
PMID: 26629857 DOI: 10.1016/j.ejmech.2015.11.021
Abstract

Aminopeptidase N (APN/CD13) over-expressed on tumor cells and tumor microenvironment, plays critical roles in tumor invasion, metastasis and 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 7a had the most potent inhibitory activity against APN with the IC50 value of 20 nM, which could be used for further Anticancer agent research.

Keywords

Aminopeptidase N; Inhibitors; Leucine ureido derivatives; Synthesis.

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