# Glycosidase-activated prodrugs of a cytotoxic iron chelator for targeted cancer therapy

## TL;DR

Researchers designed new prodrugs that release a cancer-fighting iron chelator only in cancer cells, showing selective toxicity.

## Contribution

The study introduces glycosidase-activated prodrugs of deferasirox with cancer cell-specific cytotoxicity.

## Key findings

- Glycosidase activation of prodrugs occurred within 24 hours.
- Derivative 3a showed selective toxicity against OvCar-3 cells.
- Low activity was observed against fibroblast control cells.

## Abstract

New glycoside-prodrugs based on the iron chelator deferasirox were designed. Selective enzymatic activation by glycosidases was observed within 24 hours, accompanied by cancer cell-selective cytotoxicity. Notably, derivative 3a, bearing a β-d-galactose moiety, showed promising selective activity against galactosidase overexpressing OvCar-3 cells (IC50 9.1 ± 1.6 μM) while maintaining low activity against fibroblast control GM5756 cells (IC50 > 100 μM).

New glycoside-conjugated prodrugs based on the iron chelator deferasirox were designed and their selective cleavage by glycosidases as well as cancer cell line-specific toxicity was demonstrated.