Design, synthesis and biological evaluation of novel diaryl ethers bearing a pyrimidine motif as human Pin1 inhibitors / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1266-1272, 2013.
Artigo
em Chinês
| WPRIM
| ID: wpr-259484
ABSTRACT
Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) belongs to peptidyl-prolyl cis-trans isomerase (PPIase) and is a novel promising anticancer target. Based on the lead structure of benzophenone, a series of novel diarylether derivatives containing a pyrimidine ring were designed and synthesized. The inhibitory activities on Pin1 of compounds 5a-5d and 6a-6i were evaluated by a protease-coupled enzyme assay. Of all the evaluated compounds, 6 compounds displayed inhibitory activities. Molecular docking was performed using FlexX algorithm to explore the binding mode of the active molecules.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Farmacologia
/
Pirimidinas
/
Relação Estrutura-Atividade
/
Desenho de Fármacos
/
Estrutura Molecular
/
Química
/
Peptidilprolil Isomerase
/
Concentração Inibidora 50
/
Inibidores Enzimáticos
/
Éteres
Limite:
Humanos
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2013
Tipo de documento:
Artigo
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