Exploring the C^N^C theme: Synthesis and biological properties of tridentate cyclometalated gold(III) complexes. Issue 20 (15th October 2017)

• Record Type: Journal Article
• Authors: Jürgens, Sophie; Scalcon, Valeria; Estrada-Ortiz, Natalia; Folda, Alessandra; Tonolo, Federica; Jandl, Christian; Browne, Duncan L.; Rigobello, Maria Pia; Kühn, Fritz E.; Casini, Angela
• Is Part Of: Bioorganic & medicinal chemistry. Volume 25:Issue 20(2017)
• Page Start: 5452
• Page End: 5460
• Publication Date: 2017-10-15
• Subjects: Gold(III) complexes -- Cyclometalation -- Anticancer agents -- Thioredoxin reductase -- Thiols; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2017.08.001
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: 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.