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.
Article
Dans Chinois
| 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.
Texte intégral:
Disponible
Indice:
WPRIM (Pacifique occidental)
Sujet Principal:
Pharmacologie
/
Pyrimidines
/
Relation structure-activité
/
Conception de médicament
/
Structure moléculaire
/
Chimie
/
Peptidylpropyl isomerase
/
Concentration inhibitrice 50
/
Antienzymes
/
Éthers
Limites du sujet:
Humains
langue:
Chinois
Texte intégral:
Acta Pharmaceutica Sinica
Année:
2013
Type:
Article
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