title: 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.
authors.affiliation: Department of Medical and Clinical Biochemistry, Faculty of Medicine, Pavol Jozef Šafárik University in Košice, Tr. SNP 1, 040 66, Košice, Slovak Republic.
authors.forename: Vašková
authors.initials: V
authors.lastname: Janka
authors.affiliation: Department of Medical and Clinical Biochemistry, Faculty of Medicine, Pavol Jozef Šafárik University in Košice, Tr. SNP 1, 040 66, Košice, Slovak Republic.
authors.forename: Daniel
authors.initials: D
authors.lastname: Žatko
authors.affiliation: Department of Medical and Clinical Biochemistry, Faculty of Medicine, Pavol Jozef Šafárik University in Košice, Tr. SNP 1, 040 66, Košice, Slovak Republic.
authors.forename: Vaško
authors.initials: V
authors.lastname: Ladislav
authors.affiliation: Institute of Pharmaceutical Chemistry, Faculty of Medicine, University of Pécs, Rokus u. 2, Pécs, Hungary.
authors.forename: Perjési
authors.initials: P
authors.lastname: Pál
authors.affiliation: Department of Biology, Faculty of Humanities and Natural Science, University of Prešov in Prešov, 17th November Street 1, 081 16, Prešov, Slovak Republic.
authors.forename: Poráčová
authors.initials: P
authors.lastname: Janka
authors.affiliation: Department of Experimental Medicine, Faculty of Medicine, Pavol Jozef Šafárik University in Košice, Tr. SNP 1, 040 66, Košice, Slovak Republic. gabriela.mojzisova@upjs.sk.
authors.forename: Mojžišová
authors.initials: M
authors.lastname: Gabriela
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D000975:Antioxidants / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor / Q000187:drug effects; D047188:Chalcones / Q000737:chemistry / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D005296:Ferrous Compounds / Q000737:chemistry; D005978:Glutathione / Q000378:metabolism; D006801:Humans; D006861:Hydrogen Peroxide / Q000378:metabolism; D020128:Inhibitory Concentration 50; D008297:Male; D000075163:Metallocenes; D008930:Mitochondria, Liver / Q000187:drug effects / Q000378:metabolism; D015394:Molecular Structure; D017208:Rats, Wistar; D013482:Superoxide Dismutase / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D000975:Antioxidants; D047188:Chalcones; D005296:Ferrous Compounds; D000075163:Metallocenes; D006861:Hydrogen Peroxide; D013482:Superoxide Dismutase; D005978:Glutathione; C004998:ferrocene
keywords: Anticancer agents; Antiproliferative effects; Chalcone; Cytotoxic; Ferrocene