Evaluation of perylenediimide derivatives for potential therapeutic benefits on cancer chemotherapy.
Chem Biol Drug Des
; 80(5): 675-81, 2012 Nov.
Article
de En
| MEDLINE
| ID: mdl-22834711
ABSTRACT
Perylene derivatives, known to have potential therapeutic benefits on particular cancer types as photosensitizers, may also function as small-molecule inhibitors with promising therapeutic value for diverse diseases. This recently recognized biological activity was attributed to their capacity to modulate the function of various enzymes as biological targets in vitro. Although the inhibitory activity on glutathione transferase and Src tyrosine kinase is important in determining the anticancer potential of compounds for target-specific drug design and development, to date, there are no successful inhibitors of this kind. Moreover, there are only a few studies about the effects of perylene derivatives on glutathione transferase and various kinases. In this study, four novel perylene compounds, N,N'-disubstituted perylenediimides and their 1,7-dibromo derivatives, were synthesized and evaluated for their biological activities. Here, among the compounds analyzed, one of them was identified with strong glutathione transferase inhibition and two with dual activity for both glutathione transferase and c-src inhibition. These results revealed that perylene derivatives may be employed as potential chemosensitizers to prevent chemotherapy-dependent drug resistance and identified as prospective anticancer agents with dual activity on both glutathione transferase and c-src enzymes.
Texte intégral:
1
Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Pérylène
/
Src-Family kinases
/
Inhibiteurs de protéines kinases
/
Glutathione transferase
/
Imides
/
Tumeurs
Limites:
Humans
Langue:
En
Journal:
Chem Biol Drug Des
Sujet du journal:
BIOQUIMICA
/
FARMACIA
/
FARMACOLOGIA
Année:
2012
Type de document:
Article
Pays d'affiliation:
Turquie