Discovery of bepridil as a valuable lead compound with potent p53-MDM2 inhibitory activity / 药学实践杂志
Journal of Pharmaceutical Practice
; (6): 126-129, 2021.
Article
de Zh
| WPRIM
| ID: wpr-875671
Bibliothèque responsable:
WPRO
ABSTRACT
Objective To find novel lead compounds as p53-MDM2 inhibitors by drug repurposing strategy. Methods The p53-MDM2 inhibitory activities of compounds were determined by FP and western blotting. MTT method was used to determine the in-vitro antitumor activities. The metabolites in human liver microsomes were tested. Results Bepridil showed excellent in-vitro anti-tumor activity and strong p53-MDM2 protein binding inhibitory activity, which can significantly reduce the expression of MDM2 protein in a dose-dependent manner. The metabolites in human liver microsomes are mainly benzene ring hydroxyl mono-oxidation metabolites. Conclusion Bepridil can be used as a lead compound for p53-MDM2 protein binding small molecule inhibitors for subsequent structural optimization design studies.
Texte intégral:
1
Base de données:
WPRIM
Langue:
Zh
Journal:
Journal of Pharmaceutical Practice
Année:
2021
Type de document:
Article