New 8-hydroxyquinoline galactosides. the role of the sugar in the antiproliferative activity of copper(II) ionophores

Valentina Oliveri, Maurizio Viale, Cinzia Aiello, Graziella Vecchio

Research output: Contribution to journalArticle


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.

Original languageEnglish
Pages (from-to)101-108
Number of pages8
JournalJournal of Inorganic Biochemistry
Publication statusPublished - 2015



  • Clioquinol
  • Copper
  • Galactoside
  • Ionophore

ASJC Scopus subject areas

  • Biochemistry
  • Inorganic Chemistry

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