4.7 Article

Exploring the theme: Synthesis and biological properties of tridentate cyclometalated gold(III) complexes

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 25, Issue 20, Pages 5452-5460

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2017.08.001

Keywords

Gold(III) complexes; Cyclometalation; Anticancer agents; Thioredoxin reductase; Thiols

Funding

  1. Cardiff University
  2. Technische Universitat Munchen (TUM) Graduate School
  3. Department of Sciences, Technology, and Innovation COLCIENCIAS (Colombia)
  4. TUM - Institute for Advanced Study - German Excellence Initiative
  5. European Union [291763]

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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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