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Anti-Cancer N-Heterocyclic Carbene Complexes of Gold(III), Gold(I) and Platinum(II)

Thiol “Switch-on” Fluorescent Probes, Thioredoxin Reductase Inhibitors and Endoplasmic Reticulum Targeting Agents

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  • © 2016

Overview

  • by The University of Hong Kong as an outstanding Ph.D. thesis
  • reviews the current status of gold- and platinum-based anti-cancer agents
  • Highlights the significant advances made in the area of metal-based anti-cancer agents
  • Includes original drug design, drug synthesis, cell-based bio-experiments and animal-based studies
  • Includes supplementary material: sn.pub/extras

Part of the book series: Springer Theses (Springer Theses)

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Table of contents (6 chapters)

Keywords

About this book

This thesis focuses on the development of gold- and non-classical platinum-based anti-cancer agents that display distinctively different anti-cancer mechanisms compared to the commonly used cisplatin. These metal complexes contain N-heterocyclic carbene (NHC) ligands which are able to form strong M-C(NHC) bonds, conferring high stability and favorable lipophilicity, reactivity and binding specificity of metal complexes on biomolecules. The author demonstrates significant advances made in anti-cancer gold(III), gold(I) and platinum(II) complexes. Detailed chemical synthesis, in vitro and/or in vivo anti-cancer activities are clearly presented including: (i) a class of Au(III) complexes containing a highly fluorescent N^N^N ligand and NHC ligand that simultaneously act as fluorescent thiol “switch-on” probes and anti-cancer agents; (ii) a dinuclear gold(I) complex with a mixed diphosphine and bis(NHC) ligand displaying favorable stability and showing significant inhibition of tumor growth in two independent mice models with no observable side effects; and (iii) a panel of stable luminescent cyclometalated platinum(II) complexes exhibiting high specificity to localize to the endoplasmic reticulum (ER) domain, inducing ER stress and cell apoptosis. These works highlight the clinical potential that gold and platinum complexes offer for cancer treatment.

Authors and Affiliations

  • Department of Chemistry, The University of Hong Kong, Hong Kong, Hong Kong

    Taotao Zou

About the author

Bibliographic Information

  • Book Title: Anti-Cancer N-Heterocyclic Carbene Complexes of Gold(III), Gold(I) and Platinum(II)

  • Book Subtitle: Thiol “Switch-on” Fluorescent Probes, Thioredoxin Reductase Inhibitors and Endoplasmic Reticulum Targeting Agents

  • Authors: Taotao Zou

  • Series Title: Springer Theses

  • DOI: https://doi.org/10.1007/978-981-10-0657-9

  • Publisher: Springer Singapore

  • eBook Packages: Chemistry and Materials Science, Chemistry and Material Science (R0)

  • Copyright Information: Springer Science+Business Media Singapore 2016

  • Hardcover ISBN: 978-981-10-0656-2Published: 02 March 2016

  • Softcover ISBN: 978-981-10-9221-3Published: 25 April 2018

  • eBook ISBN: 978-981-10-0657-9Published: 19 February 2016

  • Series ISSN: 2190-5053

  • Series E-ISSN: 2190-5061

  • Edition Number: 1

  • Number of Pages: XIII, 164

  • Number of Illustrations: 100 b/w illustrations, 79 illustrations in colour

  • Topics: Inorganic Chemistry, Medicinal Chemistry, Molecular Medicine, Cancer Research

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