2. Academic Validation
  3. Novel potent 2,5-pyrrolidinedione peptidomimetics as aminopeptidase N inhibitors. Design, synthesis and activity evaluation

Novel potent 2,5-pyrrolidinedione peptidomimetics as aminopeptidase N inhibitors. Design, synthesis and activity evaluation

  • Bioorg Med Chem Lett. 2012 Jan 15;22(2):850-3. doi: 10.1016/j.bmcl.2011.12.048.
Qianbin Li 1,  Hao Fang,  Xuejian Wang,  Gaoyun Hu,  Qiang Wang,  Wenfang Xu
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Central South University, 172 Tongzipo Road, 410013 Changsha, Hu'nan, China. qbli@csu.edu.cn
PMID: 22206607 DOI: 10.1016/j.bmcl.2011.12.048
Abstract

A series of novel Aminopeptidase N inhibitors with 2,5-pyrrolidinedione scaffold were chemically synthesized. Their preliminary biological activities in Enzyme kinetics and cell assay in vitro and anti-metastasis profile in vivo were also evaluated. The results indicated that all the compounds displayed potent inhibitory activity against Aminopeptidase N. Compound 8f inhibited Aminopeptidase N activity with IC(50) value of 1.0μM and displayed better activity profile in vivo than that of bestatin.

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