Is the way to fight cancer paved with gold? Metal-based carbene complexes with multiple and fascinating biological features

Domenico Iacopetta, Camillo Rosano, Marco Sirignano, Annaluisa Mariconda, Jessica Ceramella, Marco Ponassi, Carmela Saturnino, Maria Stefania Sinicropi, Pasquale Longo

Research output: Contribution to journalArticlepeer-review

Abstract

Herein, we report the synthesis and the multiple anti-tumor properties of new gold and silver carbene complexes. The chemical modifications, grounded on our previous studies, led us to identify a good lead complex, gold-based, whose biological features are very exciting and promising in the anti-cancer research and could be further developed. Indeed, the bis-[4,5-dichloro-(N-methyl-N’(2-hydroxy-2-phenyl)ethyl-imidazole-2-ylidene)gold(I)]+ [dichloro-gold] (AuL7) complex possesses the ability to interfere with at least three important and different intracellular targets, namely the human topoisomerases I and II and tubulin, which are able to modulate metabolic processes not directly correlated each other. We proved that the modifications of the ligands structure in AuL7, with respect to another already published complex, i.e., bis-[4,5-dichloro-(N-methyl-N’(cyclopentane-2ol)-imidazole-2-ylidine)gold(I)]+[dichloro-gold] (AuL4), produce a different behavior toward tubulin-polymerization process, since AuL7 is a tubulin-polymerization inhibitor and AuL4 a stabilizer, with the final same result of hampering the tumor growth. Taken together, our outcomes designate AuL7 as a promising compound for the development of multi-targeted anti-cancer therapies.

Original languageEnglish
Article number91
JournalPharmaceuticals
Volume13
Issue number5
DOIs
Publication statusPublished - May 11 2020

Keywords

  • Carbene complexes
  • Docking studies
  • Human topoisomerases I and II
  • Tubulin
  • Women cancers

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmaceutical Science

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