期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 25, 期 20, 页码 5452-5460出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2017.08.001
关键词
Gold(III) complexes; Cyclometalation; Anticancer agents; Thioredoxin reductase; Thiols
资金
- Cardiff University
- Technische Universitat Munchen (TUM) Graduate School
- Department of Sciences, Technology, and Innovation COLCIENCIAS (Colombia)
- TUM - Institute for Advanced Study - German Excellence Initiative
- European Union [291763]
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. (C) 2017 Elsevier Ltd. All rights reserved.
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