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

Bioorganic & Medicinal Chemistry Letters
2012.0

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.

Knowledge Graph

Similar Paper

Novel potent 2,5-pyrrolidinedione peptidomimetics as aminopeptidase N inhibitors. Design, synthesis and activity evaluation
Bioorganic & Medicinal Chemistry Letters 2012.0
Novel cyclic-imide peptidomimetics as aminopeptidase N inhibitors. Design, chemistry and activity evaluation. Part I
European Journal of Medicinal Chemistry 2009.0
Novel cyclic-imide peptidomimetics as aminopeptidase N inhibitors. Structure-based design, chemistry and activity evaluation. II
European Journal of Medicinal Chemistry 2010.0
Novel 3-galloylamido-N′-substituted-2,6-piperidinedione-N-acetamide peptidomimetics as metalloproteinase inhibitors
Bioorganic & Medicinal Chemistry Letters 2007.0
Novel 3-phenylpropane-1,2-diamine derivates as inhibitors of aminopeptidase N (APN)
Bioorganic & Medicinal Chemistry 2008.0
Novel indoline-2,3-dione derivatives as inhibitors of aminopeptidase N (APN)
Bioorganic & Medicinal Chemistry 2013.0
Design, synthesis, and preliminary studies of the activity of novel derivatives of N-cinnamoyl-l-aspartic acid as inhibitors of aminopeptidase N/CD13
Bioorganic & Medicinal Chemistry 2009.0
Novel aminopeptidase N (APN/CD13) inhibitors derived from 3-phenylalanyl-N′-substituted-2,6-piperidinedione
Bioorganic & Medicinal Chemistry 2010.0
Novel aminopeptidase N inhibitors derived from antineoplaston AS2–5 (Part II)
Bioorganic & Medicinal Chemistry 2009.0
Design, synthesis and SAR studies of tripeptide analogs with the scaffold 3-phenylpropane-1,2-diamine as aminopeptidase N/CD13 inhibitors
Bioorganic & Medicinal Chemistry 2009.0