Antitumor effects of binuclear ferrocene derivatives

Abstract

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.

Antimalarial, Anti-trypanosomiasis, Anti-HIV and Cytotoxicity Studies of Some Ferrocenyl Schiff bases

“…All the compounds (1-12) showed low toxicity because %cell viability was above 50%. This is not surprising because it had earlier been reported that ferrocenyl derived compounds do possess low toxicity [46]- [48]. …”

Antineoplastic activity of polyaspartamide-ferrocene conjugates

“…22 Promising activity behavior was reported independently for the tetrachloroferrate 23 and for the triiodide, 24 with therapeutic indices appreciably larger than determined for cisplatin. Lastly, activity was shown by certain azole derivaties of ferrocene which could potentially exist in a form featuring a cationic site.…”

Synthesis and Electrochemical Properties of N-(Ferrocenylmethyl)Aminobenzonitrile and N-(Ferrocenylmethyl)Nitroaniline Derivatives

“…The incorporation of (methylamino)benzonitrile and N-methylnitroaniline in a ferrocene moiety could provide new derivatives with important biological activities since several ferrocene derivatives have already been shown to be active against a number of tumors [17][18][19]. Herein we report the synthesis, characterization and electrochemical behavior of a series of N-(ferrocenylmethyl)aminobenzonitrile and N-(ferrocenylmethyl)nitroaniline derivatives which combiFne the ferrocene moiety with (methylamino)benzonitrile and N-methylnitroaniline groups.…”