8-Hydroxyquinoline derivatives and their metal complexes have recently awakened interest as promising therapeutic agents in cancer therapy. We have previously synthesized and evaluated glucoconjugated 8-hydroxyquinolines as copper ionophores activated by β-glucosidases.In order to further evaluate the crucial role of the sugar, we designed and synthesized a series of new galactoconjugates of 8-hydroxyquinolines and investigated their biological properties in comparison with the 8-hydroxyquinoline analogs. The effect of copper(II) ions on their biological activities was evaluated. In particular, two compounds possess a pharmacologically relevant antiproliferative activity against specific tumor cells in the presence of copper(II) ions. Furthermore, the antiproliferative activity of the selected galactosides was successfully investigated in the presence of β-galactosidase as a preliminary model of antibody directed enzyme prodrug therapy.
New 8-hydroxyquinoline galactosides. The role of the sugar in the antiproliferative activity of copper(II) ionophores
OLIVERI, VALENTINA;VECCHIO, Graziella
2015-01-01
Abstract
8-Hydroxyquinoline derivatives and their metal complexes have recently awakened interest as promising therapeutic agents in cancer therapy. We have previously synthesized and evaluated glucoconjugated 8-hydroxyquinolines as copper ionophores activated by β-glucosidases.In order to further evaluate the crucial role of the sugar, we designed and synthesized a series of new galactoconjugates of 8-hydroxyquinolines and investigated their biological properties in comparison with the 8-hydroxyquinoline analogs. The effect of copper(II) ions on their biological activities was evaluated. In particular, two compounds possess a pharmacologically relevant antiproliferative activity against specific tumor cells in the presence of copper(II) ions. Furthermore, the antiproliferative activity of the selected galactosides was successfully investigated in the presence of β-galactosidase as a preliminary model of antibody directed enzyme prodrug therapy.File | Dimensione | Formato | |
---|---|---|---|
New 8-hydroxyquinoline galactosides.pdf
solo gestori archivio
Tipologia:
Versione Editoriale (PDF)
Licenza:
NON PUBBLICO - Accesso privato/ristretto
Dimensione
712.38 kB
Formato
Adobe PDF
|
712.38 kB | Adobe PDF | Visualizza/Apri |
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.