Exploring the C^N^C theme: synthesis and biological properties of tridentate cyclometalated gold(III) complexes

Publication date: Available online 9 August 2017
Source:Bioorganic & Medicinal Chemistry
Author(s): Sophie Jürgens, Valeria Scalcon, Natalia Estrada-Ortiz, Alessandra Folda, Federica Tonolo, Christian Jandl, Duncan L. Browne, Maria Pia Rigobello, Fritz E. Kühn, Angela Casini
A family of cyclometalated Au(III) complexes featuring a tridentate C^N^C scaffold has been synthesized and characterized. Microwave assisted synthesis of the ligands has also been exploited and optimized. The biological properties of the thus formed compounds have been studied in cancer cells and demonstrate generally moderate antiproliferative effects. Initial mechanistic insights have also been gained on the gold complex [Au(C^N^C)(GluS)] (3), and support the idea that the thioredoxin system may be a target for this family of compounds together with other relevant intracellular thiol-containing molecules.

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