Applying a Trojan Horse Strategy to Ruthenium Complexes in the Pursuit of Novel Antibacterial Agents

• Published in: Organometallics Vol. 37; no. 6; pp. 915 - 923
• Main Authors: Laurent, Quentin, Batchelor, Lucinda K, Dyson, Paul J
• Format: Journal Article
• Language: English
• Published: American Chemical Society 26.03.2018
• ISSN: 0276-7333; 1520-6041
• DOI: 10.1021/acs.organomet.7b00885

Siderophores are iron chelators secreted by bacteria to scavenge iron­(III) from their surrounding environment. They possess their own internalization pathway that is sufficiently unselective to be hijacked, making them suitable for Trojan Horse strategy applications. A commercially available siderophore, deferoxamine B (DFO), was derivatized at the primary amine with carboxylic acids bearing different ligands to afford mono- and bidentate complexes with ruthenium as well as a RAPTA-like complex in which DFO is tethered to the coordinated arene ring. These compounds were tested for antibacterial activity against key ESKAPE pathogens, and antiproliferative studies against healthy (HEK-293) and tumoral (A2780) human cells were performed. Some of the complexes displayed interesting dual anticancer and antibacterial properties. Combining these two properties within a single compound is desirable as patients treated for cancer have a weakened ability for fighting infections.