Anti-Cancer Drug : association of iron chelator and polyamine

The goal of the new concept, named Quilamine, is to target two processus which are overactive in tumor cells: Iron metabolism and Polyamine Transport System (PTS).

Molecule description: Quilamine is composed of 8-hydroxyquinoleine (C9H7NO) scaffold linked to linear polyamine vectors. HQ1-44, the most promising one, presents a homospermidine moiety and was proved to be highly taken up by the PTS and to display an efficient antiproliferative activity.

Mode of action: Quilamines were designed to target tumor cells expressing an overactive PTS.

• High complexation capacity with iron while much weaker complexes were formed with other cations
• Strong tridentate ligand for iron (III), especially in the form of a 1:2 complex
• Antiproliferative activity similar to Cisplatin (in vivo results)
• No side-effect (in vivo in Swiss nude mice)