Identification of gallic acid based glycoconjugates as a novel tubulin polymerization inhibitors.
Org Biomol Chem
; 14(4): 1338-58, 2016 Jan 28.
Article
de En
| MEDLINE
| ID: mdl-26659548
ABSTRACT
A novel class of gallic acid based glycoconjugates were designed and synthesized as potential anticancer agents. Among all the compounds screened, compound 2a showed potent anticancer activity against breast cancer cells. The latter resulted in tubulin polymerization inhibition and induced G2/M cell cycle arrest, generation of reactive oxygen species, mitochondrial depolarization and subsequent apoptosis in breast cancer cells. In addition, ultraviolet-visible spectroscopy and fluorescence quenching studies of the compound with tubulin confirmed direct interaction of compounds with tubulin. Molecular modeling studies revealed that it binds at the colchicine binding site in tubulin. Further, 2a also exhibited potent in vivo anticancer activity in LA-7 syngeneic rat mammary tumor model. Current data projects its strong candidature to be developed as anticancer agent.
Texte intégral:
1
Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Tubuline
/
Glycoconjugués
/
Modulateurs de la polymérisation de la tubuline
/
Polymérisation
/
Acide gallique
/
Antinéoplasiques
Type d'étude:
Diagnostic_studies
Limites:
Animals
/
Female
/
Humans
Langue:
En
Journal:
Org Biomol Chem
Sujet du journal:
BIOQUIMICA
/
QUIMICA
Année:
2016
Type de document:
Article