RT Journal Article
T1 N-Heterocyclic Carbene Iron Complexes as Anticancer Agents: In Vitro and In Vivo Biological Studies
A1 Lenis Rojas, Óscar
A1 Cordeiro, Sandra
A1 Araujo Fernández, Jhonathan Angel
A1 Rubiolo Gaytán, Juan Andrés
A1 Cabezas Sáinz, Pablo
A1 Sánchez Piñón, Laura
A1 Fernandes, Alexandra
A1 Royo, Beatriz
A1 Horta Meireles, Marta
A1 Fernández Vila, Sabela
K1 N-heterocyclic carbene
K1 Iron(II)–NHC complexes
K1 Anticancer activity
K1 Zebrafish
AB 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.
PB MDPI
SN 1420-3049
YR 2021
FD 2021-09-12
LK http://hdl.handle.net/10347/32017
UL http://hdl.handle.net/10347/32017
LA eng
NO Lenis-Rojas, O.A.; Cordeiro, S.; Horta-Meireles, M.; Fernández, J.A.A.; Fernández Vila, S.; Rubiolo, J.A.; Cabezas-Sainz, P.; Sánchez, L.; Fernandes, A.R.; Royo, B. N-Heterocyclic Carbene Iron Complexes as Anticancer Agents: In Vitro and In Vivo Biological Studies. Molecules 2021, 26, 5535. https://doi.org/10.3390/molecules26185535
NO This research was funded by national funds through FCT–Fundação para a Ciência e a Tecnologia, I.P., Project MOSTMICRO-ITQB (UIDB/04612/2020 and UIDP/04612/2020, Project LISBOA-01-0145-FEDER-007660), and national funds through FCT, POPH-Programa Operacional Potencial Humano, and FSE (European Social Fund) for the CEEC 2017 Initiative CEECIND/04566/2017. Additionally, this work was supported by the Portuguese Foundation for Science and Technology (FCT—Fundação para a Ciência e a Tecnologia) for funding through projects PEst 2015 2020, UID/Multi/04349/2013, RECI/QEQ-QIN/0189/2012, and UID/QUI/00100/2020. This work was financed by national funds from FCT—Fundação para a Ciência e a Tecnologia, I.P., in the scope of the project UIDP/04378/2020 and UIDB/04378/2020 of the Research Unit on Applied Molecular Biosciences—UCIBIO and the project LA/P/0140/2020 of the Associate Laboratory Institute for Health and Bioeconomy—i4HB. The NMR spectrometers at CERMAX are integrated with the national NMR Network and partially supported through project 022162.
DS Minerva
RD 28 abr 2026