Chemistry, structure, and biological roles of Au-NHC complexes as TrxR inhibitors

Bioorg Chem. 2020 Jan:95:103552. doi: 10.1016/j.bioorg.2019.103552. Epub 2019 Dec 24.

Abstract

In recent years, the preparation of metal complexes and the introduction of biologically active organometalic compounds are new strategies in drug development. For this purpose, generally N-heterocyclic pharmaceutical agents have been used as promising nuclei. Au-containing N-heterocyclic carbene (Au-NHC) derivatives are among the compounds used for this purpose, and their enzyme inhibition, antioxidant activity, antimicrobial and anticancer properties are widely studied. In these studies, the anticancer property of Au-NHC complexes is the most widely studied area. The common result in different studies has been revealed that mitochondrial thioredoxin reductases (TrxR) inhibition is the main pathway in the powerful anticancer effect of many Au-NHC complexes. In TrxR inhibition, the high affinity of gold to sulfur is considered to be the main component of the effect. This review includes the discussions releated to the anticancer activities and TrxR inhibition properties of Au-NHC compounds.

Keywords: Anticancer activity; Au-NHC complexes; Enzyme; TrxR inhibitors.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Gold / chemistry*
  • Heterocyclic Compounds / chemistry
  • Heterocyclic Compounds / pharmacology*
  • Humans
  • Thioredoxin-Disulfide Reductase / antagonists & inhibitors*

Substances

  • Antineoplastic Agents
  • Heterocyclic Compounds
  • Gold
  • Thioredoxin-Disulfide Reductase