PUBLICATION
N-Heterocyclic Carbene Iron Complexes as Anticancer Agents: In Vitro and In Vivo Biological Studies
- Authors
- Lenis-Rojas, O.A., Cordeiro, S., Horta-Meireles, M., Fernández, J.A.A., Fernández Vila, S., Rubiolo, J.A., Cabezas-Sainz, P., Sanchez, L., Fernandes, A.R., Royo, B.
- ID
- ZDB-PUB-210929-17
- Date
- 2021
- Source
- Molecules 26(18): (Journal)
- Registered Authors
- Cabezas-Sainz, Pablo
- Keywords
- N-heterocyclic carbene, anticancer activity, iron(II)–NHC complexes, zebrafish
- MeSH Terms
-
- Animals
- Antineoplastic Agents/chemistry*
- Antineoplastic Agents/pharmacology*
- Antineoplastic Agents/therapeutic use
- Antineoplastic Agents/toxicity
- Cell Line, Tumor
- Cell Survival/drug effects
- Cisplatin/pharmacology
- Drug Screening Assays, Antitumor
- Fibroblasts/drug effects
- Heterocyclic Compounds/chemistry*
- Heterocyclic Compounds/pharmacology*
- Heterocyclic Compounds/therapeutic use
- Heterocyclic Compounds/toxicity
- Humans
- Inhibitory Concentration 50
- Iron Compounds/chemistry*
- Iron Compounds/pharmacology*
- Iron Compounds/therapeutic use
- Iron Compounds/toxicity
- Methane/analogs & derivatives*
- Methane/chemistry
- Neoplasms/drug therapy
- Neoplasms/pathology
- Xenograft Model Antitumor Assays
- Zebrafish
- PubMed
- 34577006 Full text @ Molecules
Citation
Lenis-Rojas, O.A., Cordeiro, S., Horta-Meireles, M., Fernández, J.A.A., Fernández Vila, S., Rubiolo, J.A., Cabezas-Sainz, P., Sanchez, L., Fernandes, A.R., Royo, B. (2021) N-Heterocyclic Carbene Iron Complexes as Anticancer Agents: In Vitro and In Vivo Biological Studies. Molecules. 26(18):.
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.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping