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.
Original language | English |
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Pages (from-to) | 101-108 |
Number of pages | 8 |
Journal | Journal of Inorganic Biochemistry |
Volume | 142 |
DOIs | |
Publication status | Published - 2015 |
Keywords
- ADEPT
- Clioquinol
- Copper
- Galactoside
- Ionophore
ASJC Scopus subject areas
- Biochemistry
- Inorganic Chemistry