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© 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.

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.

Details

Title
N-Heterocyclic Carbene Iron Complexes as Anticancer Agents: In Vitro and In Vivo Biological Studies
Author
Lenis-Rojas, Oscar A 1 ; Cordeiro, Sandra 2 ; Horta-Meireles, Marta 1 ; Jhonathan Angel Araujo Fernández 3 ; Sabela Fernández Vila 4 ; Juan Andrés Rubiolo 5 ; Cabezas-Sainz, Pablo 4   VIAFID ORCID Logo  ; Sanchez, Laura 6   VIAFID ORCID Logo  ; Fernandes, Alexandra R 2   VIAFID ORCID Logo  ; Royo, Beatriz 1   VIAFID ORCID Logo 

 ITQB NOVA, Instituto de Tecnologia Química e Biológica António Xavier, Av. da República, 2780-157 Oeiras, Portugal; [email protected] 
 UCIBIO, Departamento Ciências da Vida, NOVA School of Science and Technology, NOVA University, Campus de Caparica, 2829-516 Caparica, Portugal; [email protected]; Associate Laboratory i4HB—Institute for Health and Bioeconomy, NOVA School of Science and Technology, NOVA University, 2819-516 Caparica, Portugal 
 Departamento de Zoología Genética y Antropología Física, Facultad de Veterinaria, Universidad de Santiago de Compostela, Campus de Lugo, 27002 Lugo, Spain; [email protected] (J.A.A.F.); [email protected] (S.F.V.); [email protected] (J.A.R.); [email protected] (P.C.-S.); [email protected] (L.S.); Laboratory of Zebrafish, Department of Medical Genetics and Genomic Medicine—School of Medical Sciences, University of Campinas (UNICAMP), Campinas 13083-970, SP, Brazil 
 Departamento de Zoología Genética y Antropología Física, Facultad de Veterinaria, Universidad de Santiago de Compostela, Campus de Lugo, 27002 Lugo, Spain; [email protected] (J.A.A.F.); [email protected] (S.F.V.); [email protected] (J.A.R.); [email protected] (P.C.-S.); [email protected] (L.S.) 
 Departamento de Zoología Genética y Antropología Física, Facultad de Veterinaria, Universidad de Santiago de Compostela, Campus de Lugo, 27002 Lugo, Spain; [email protected] (J.A.A.F.); [email protected] (S.F.V.); [email protected] (J.A.R.); [email protected] (P.C.-S.); [email protected] (L.S.); Facultad de Ciencias Bioquímicas y Farmacéuticas-Centro Científico y Tecnológico Acuario del Río Paraná, Universidad Nacional de Rosario, Rosario 2000, Argentina 
 Departamento de Zoología Genética y Antropología Física, Facultad de Veterinaria, Universidad de Santiago de Compostela, Campus de Lugo, 27002 Lugo, Spain; [email protected] (J.A.A.F.); [email protected] (S.F.V.); [email protected] (J.A.R.); [email protected] (P.C.-S.); [email protected] (L.S.); Preclinical Animal Models Group, Health Research Institute of Santiago de Compostela (IDIS), 5706 Santiago de Compostela, Spain 
First page
5535
Publication year
2021
Publication date
2021
Publisher
MDPI AG
e-ISSN
14203049
Source type
Scholarly Journal
Language of publication
English
ProQuest document ID
2576400288
Copyright
© 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.