N-Heterocyclic Carbene Iron Complexes as Anticancer Agents: In Vitro and In Vivo Biological Studies

被引：17

作者：

Lenis-Rojas, Oscar A. ^{[1
]}

Cordeiro, Sandra ^{[2
,3
]}

Horta-Meireles, Marta ^{[1
]}

Araujo Fernandez, Jhonathan Angel ^{[4
,5
]}

Fernandez Vila, Sabela ^{[4
]}

Andres Rubiolo, Juan ^{[4
,6
]}

Cabezas-Sainz, Pablo ^{[4
]}

Sanchez, Laura ^{[4
,7
]}

Fernandes, Alexandra R. ^{[2
,3
]}

Royo, Beatriz ^{[1
]}

机构：

[1] Inst Tecnol Quim & Biol Antonio Xavier, ITQB NOVA, Av Republ, P-2780157 Oeiras, Portugal

[2] NOVA Univ, NOVA Sch Sci & Technol, Dept Ciencias Vida, UCIBIO, Campus Caparica, P-2829516 Caparica, Portugal

[3] NOVA Univ, NOVA Sch Sci & Technol, Inst Hlth & Bioecon, Associate Lab I4HB, P-2819516 Caparica, Portugal

[4] Univ Santiago Compostela, Fac Vet, Dept Zool Genet & Antropol Fis, Campus Lugo, Lugo 27002, Spain

[5] Univ Campinas UNICAMP, Sch Med Sci, Dept Med Genet & Genom Med, Lab Zebrafish, BR-13083970 Campinas, SP, Brazil

[6] Univ Nacl Rosario, Fac Ciencias Bioquim & Farmaceut, Ctr Cientif & Tecnol Acuario Rio Parana, RA-2000 Rosario, Argentina

[7] Hlth Res Inst Santiago de Compostela IDIS, Preclin Anim Models Grp, Santiago De Compostela 5706, Spain

来源：

MOLECULES | 2021年 / 26卷 / 18期

关键词：

N-heterocyclic carbene; iron(II)-NHC complexes; anticancer activity; zebrafish; LIGANDS; PLATINUM; BEARING; GOLD;

D O I：

10.3390/molecules26185535

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页数：14

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