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.
Highlights
50% of chemotherapeutic regimens for the treatment of cancer are based on cis-platinum and its derivatives [1]
1,3‐bis(2,4,6‐trimethyl‐phenyl)imidazol‐2‐ylidene) were synthesised following the Molecules 2021, 26, 5535 procedures previously described in the literature [42,43]
These results demonstrate the potential of cyclopentadienyl iron(II) N-heterocyclic carbene (NHC)
Summary
50% of chemotherapeutic regimens for the treatment of cancer are based on cis-platinum and its derivatives [1] These compounds have achieved significant clinical benefits for some solid tumours, their efficacy has been limited by toxic side effects and the development of drug resistance [2,3,4]. Their proven antitumor activity is driving the search for new metal complexes as potential anticancer drugs [5,6,7,8].
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