Three rationally designed glucose-platinum conjugates (Glc-Pts) were synthesized and their biological activities evaluated. The Glc-Pts, 1-3, exhibit high levels of cytotoxicity toward a panel of cancer cells. The subcellular target and cellular uptake mechanism of the Glc-Pts were elucidated. For uptake into cells, Glc-Pt 1 exploits both glucose and organic cation transporters, both widely overexpressed in cancer. Compound 1 preferentially accumulates in and annihilates cancer, compared to normal epithelial, cells in vitro. Glucose-platinum conjugates for targeted delivery: A rationally designed potent glucose-platinum conjugate exploits glucose transporters, which are widely overexpressed in cancers, for internalization and selectively accumulates in and annihilates cancer cells.
- antitumor agents
- glucose transporters
- medicinal inorganic chemistry