N-heterocyclic carbene iron complexes as anticancer agents: In vitro and in vivo biological studies

Oscar A. Lenis-Rojas, Sandra Cordeiro, Marta Horta-Meireles, Jhonathan Angel Araujo Fernández, Sabela Fernández Vila, Juan Andrés Rubiolo, Pablo Cabezas-Sainz, Laura Sanchez, Alexandra R. Fernandes, Beatriz Royo

Research output: Contribution to journalArticlepeer-review

4 Citations (Scopus)
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Abstract

Cisplatin and its derivatives are commonly used in chemotherapeutic treatments of cancer, even though they suffer from many toxic side effects. The problems that emerge from the use of these metal compounds led to the search for new complexes capable to overcome the toxic side effects. Here, we report the evaluation of the antiproliferative activity of Fe(II) cyclopentadienyl complexes bearing n-heterocyclic carbene ligands in tumour cells and their in vivo toxicological profile. The in vitro antiproliferative assays demonstrated that complex Fe1 displays the highest cytotoxic activity both in human colorectal carcinoma cells (HCT116) and ovarian carcinoma cells (A2780) with IC50 values in the low micromolar range. The antiproliferative effect of Fe1 was even higher than cisplatin. Interestingly, Fe1 showed low in vivo toxicity, and in vivo analyses of Fe1 and Fe2 compounds using colorectal HCT116 zebrafish xenograft showed that both reduce the proliferation of human HCT116 colorectal cancer cells in vivo.

Original languageEnglish
Article number5535
JournalMolecules
Volume26
Issue number18
DOIs
Publication statusPublished - 12 Sept 2021

Keywords

  • Anticancer activity
  • Iron(II)–NHC complexes
  • N-heterocyclic carbene
  • Zebrafish

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