Some ferrocenyl chalcones as useful candidates for cancer treatment

Abstract

Although knowledge of cancer management is extensive, mortality is not currently declining in this area. It is therefore important to implement a long-term strategy that would aim to prevent these serious diseases. Ferrocene-related organometallic compounds are promising candidates for design of new drugs since they can exhibit much greater biological activity than their phenyl analogs. In our work, we focused on investigating the cytotoxic and antiproliferative effects of five ferrocenyl derivatives toward selected tumor cell lines. We found that some of these substances significantly reduced Jurkat cell survival and, to a lesser extent, that of the HeLa, MCF7, A549, and MDA cells. Long-term treatment of HeLa cell cultures with these agents resulted in a significant blockade of formation of tumor cell colonies. We found that one of the mechanisms of action of the compounds is likely to display an effect on the redox state of the mitochondria at a final concentration of 10(-4) and 10(-5) mol l(-1). Of the compounds tested, the indanonyl ferrocene derivative (C) was the most effective, especially via glutathione depletion. Based on the obtained results, it can be concluded that synthetic substances containing iron have potential antitumor activity.

The Synthesis and Anti-cancer Activities of Ferrocenyl Chalcones; Drug-Likeness Calculations

“…Similar antifungal activities were reported by Muskinja et al for different ferrocenyl chalcones (Muskinja et al, 2016). Janka et al prepared novel ferrocenyl chalcones and screened their anti-cancer activities against HeLa, MCF7, A549 and MDA cells and reported that they have potential antitumor activity (Janka et al, 2015).…”

Introductory Chapter: Unregulated Mitochondrial Production of Reactive Oxygen Species in Testing the Biological Activity of Compounds

“…In previous studies on various different ferrocene derivatives, some have been shown to exhibit surprisingly high toxicity and antiproliferative activity [32][33][34]. Among the unique derivatives available for study, the antiproliferative effect of the (E)-3-(ferroceneethylene)-4-chromanone was the most effective [35]. The pronounced effect of cell viability and colony formation of cancer cells in dose-dependent manner has been shown by 1,1′-bis[(1-oxoindane-2-ylidene) methyl] ferrocene.…”

Syntheses, Structural Snapshots, Solution Redox Properties, and Cytotoxic Performances of Designated Ferrocene Scaffolds Appended with Organostannyl(IV) benzoates en Route for Human Hepatic Carcinoma

“…Notably, the ferrocenyl unit was conjugated with known compounds possessing chemotherapeutic properties, e.g., adenine, , peptides, , nucleosides and nucleobases, , vitamins, , and phenols including taxoids (paclitaxel and docetaxel, antineoplastic agents), in order to have built-in efficacy. Thus, Fc as an effective bioisostere has provided a potential platform for drug design by virtue of its aforementioned properties and three-dimensional metallocene unit, which may lead to some alterations in selectivity toward biological targets, in comparison with phenyl or alkyl groups. , …”

“…Thus, Fc as an effective bioisostere has provided a potential platform for drug design by virtue of its aforementioned properties and threedimensional metallocene unit, which may lead to some alterations in selectivity toward biological targets, in comparison with phenyl or alkyl groups. 24,25 On the other hand, the last few decades have witnessed renewed research interest in organotin(IV) compounds, which poses diverse medicinal applications such as antiviral, antimicrobial, antiparasitic, antihypertensive, antihyperbilirubinemia, and anticancer activities, apart from their standard uses as biocides, catalysts, and stabilizers. 26−32 In comparison to standard drugs, the majority of organotin(IV) carboxylates discussed in the literature have shown superior anticancer activity against various cell lines.…”