Literature DB >> 26629857

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

Chunhua Ma1, Jiangying Cao2, Xuewu Liang2, Yongxue Huang2, Ping Wu3, Yingxia Li3, Wenfang Xu2, Yingjie Zhang4.   

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.
Copyright © 2015 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Aminopeptidase N; Inhibitors; Leucine ureido derivatives; Synthesis

Mesh:

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Year:  2015        PMID: 26629857     DOI: 10.1016/j.ejmech.2015.11.021

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  4 in total

1.  The Rational Design of Therapeutic Peptides for Aminopeptidase N using a Substrate-Based Approach.

Authors:  Shilvi Joshi; Lang Chen; Michael B Winter; Yi-Lun Lin; Yang Yang; Mariya Shapovalova; Paige M Smith; Chang Liu; Fang Li; Aaron M LeBeau
Journal:  Sci Rep       Date:  2017-05-02       Impact factor: 4.379

2.  Distinct Epitopes on CD13 Mediate Opposite Consequences for Cell Adhesion.

Authors:  Claudia A Garay-Canales; Ileana Licona-Limón; Enrique Ortega
Journal:  Biomed Res Int       Date:  2018-03-29       Impact factor: 3.411

3.  Aminopeptidase N Inhibitors as Pointers for Overcoming Antitumor Treatment Resistance.

Authors:  Oldřich Farsa; Veronika Ballayová; Radka Žáčková; Peter Kollar; Tereza Kauerová; Peter Zubáč
Journal:  Int J Mol Sci       Date:  2022-08-29       Impact factor: 6.208

4.  Discovery of novel non-competitive inhibitors of mammalian neutral M1 aminopeptidase (APN).

Authors:  Isel Pascual; Pedro A Valiente; Gabriela García; Mario E Valdés-Tresanco; Yarini Arrebola; Lisset Díaz; Lotfi Bounaadja; Rosa María Uribe; Mae Chappé Pacheco; Isabelle Florent; Jean-Louis Charli
Journal:  Biochimie       Date:  2017-09-28       Impact factor: 4.079

  4 in total

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