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Synthesis and molecular simulation study of furoic peptidomimetic derivatives as potent aminopeptodase N inhibitors.
Pharmazie; 73(3): 123-127, 2018 03 05.
Artigo em Inglês | MEDLINE | ID: mdl-29544557
ABSTRACT
The aminopeptidase N (APN) plays a critical role in angiogenesis and is over-expressed in tumor cells. In this paper, we report the synthesis and enzyme inhibition assay of furoic peptidomimetic compounds. These new compounds exhibit potent inhibitory ability toward APN with IC50 values lying in the micromolar level. The binding mode of inhibitors in APN active site was explained by a molecular simulation study. These data reveal that ligand coordinating with the catalytic Zn-ion is very important for inhibitory activities.

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Texto completo: Disponível Coleções: Bases de dados internacionais Base de dados: MEDLINE Idioma: Inglês Revista: Pharmazie Assunto da revista: Farmácia Ano de publicação: 2018 Tipo de documento: Artigo