On the basis of an earlier model of chemical carcinogenesis, the antitumor activity of the mono-, bi-and poly-nuclear ferrocene derivatives ferricenium tri-iodide (l), ferricenium tetrachloroferrate (2), 1,l'-diethylferricenium triiodide (3), N-(ferrocenylmethy1)hexamethylenetetramine tetrafluoroborate (4), bis(ferrocenylmethy1)benzotriazolium tetrafluoroborate (3, bis(ferroceny1-a-ethy1)benzotriazolium tetrafluoroborate (6) and bis(ferrocenylmethyl)-2-methylbenzimidazolium tetrafluoroborate (7), and the oligomer (-Fc-CH,-FC+'--CH~),~-(PF& (8) was studied in uiuo (Fc = C,,H,Fe).The tumor models studied included MCH-11 (mouse sarcoma induced by methylcholantrene), P-815 (mouse mastocytoma of DBA/2 origin) and virus-induced Raucher leukemia (RLV). The cytotoxic effects of these preparations were examined against in vitro cultured normal murine cells (line L-929). The binuclear ferrocene derivatives 5, 6 and 7 inhibited the development of experimental tumors in mice. Ferricenium tri-iodide (1) was effective in Rauscher leukemia. Kinetic dependencies for most complexes had a two-phase character: the region of inhibition of tumorogenesis was followed by a region in which the complexes accelerated the development of this process. The link between the structure of compounds 1-8 and their antitumor effects is discussed.
We analyzed the research data on antitumor effects of a wide range of ferrocene compounds and discussed possible mechanisms of their bioactivities. Current trends in the study of antican cer effects of ferrocene derivatives were considered. Promising ways in the design of low toxicity anticancer ferrocene based drugs of new generation were outlined. * Dedicated to the 60th anniversary of the A. N. Nesmeyanov Institute of Organoelement Compounds of the Russian Academy of Sciences (INEOS RAS). The review was written on the initiative and with the active participation of Yu. S. Nekrasov who served with good faith and fidelity for INEOS RAS for more than 40 years. † Deceased.
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