2. Academic Validation
  3. Novel cyclic-imide peptidomimetics as aminopeptidase N inhibitors. Design, chemistry and activity evaluation. Part I

Novel cyclic-imide peptidomimetics as aminopeptidase N inhibitors. Design, chemistry and activity evaluation. Part I

  • Eur J Med Chem. 2009 Dec;44(12):4819-25. doi: 10.1016/j.ejmech.2009.07.022.
Qianbin Li 1,  Hao Fang,  Xuejian Wang,  Liping Hu,  Wenfang Xu
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44 West Wenhua Road, 250012 Ji'nan, Shandong, PR China.
PMID: 19683842 DOI: 10.1016/j.ejmech.2009.07.022
Abstract

A series of Aminopeptidase inhibitors with cyclic-imide scaffold are described. The biological characterization for the piperidinedione analogues revealed that most compounds displayed high inhibitory activity against APN. Among which 4l and 6 showed potent inhibition against APN with the IC(50) value of 5.2 microM and 3.1 microM, respectively. In addition, 6 also displayed good activity in HL-60 cell assay and in vivo anti-metastasis assay. This interesting activity profile may also guide the design of new, specific inhibitors of target mammalian aminopeptidases with 'one-zinc' active site.

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