BACKGROUND: Often potentially good chemotherapeutic drugs find limited clinical use due to the many negative medical and physical side-effects they may exhibit. To combat these negative side-effects, new antineoplastic materials are continuously being synthesised and evaluated. Ferrocene-containing compounds under certain conditions may show appreciable anticancer activity. Some of the factors that determine this activity have been investigated. MATERIALS AND METHODS: Ferrocene-containing alcohols were tested for cytotoxicity against the HeLa cancer cell line. Cell survival was measured by means of the colorometric 3-(4,5-dimethylthiazol-2-yl)-diphenyltetrazolium bromide assay. RESULTS: The 50% lethal dosage of 4-ferrocenylbutanol was 5.72 micromol. dm(-3) and for 2-ferrocenylethanol and 3-ferrocenylpropanol it was 35.0 and 17 micromol. dm(-3) respectively while for ferrocenylmethanol IC50 was >100 micromol. dm(-3). CONCLUSION: A drug activity-structural relationship exists in that ferrocenyl drugs with longer side chains are more cytotoxic. Compounds with lower ferrocenyl group formal reduction potential are also more cytotoxic.
BACKGROUND: Often potentially good chemotherapeutic drugs find limited clinical use due to the many negative medical and physical side-effects they may exhibit. To combat these negative side-effects, new antineoplastic materials are continuously being synthesised and evaluated. Ferrocene-containing compounds under certain conditions may show appreciable anticancer activity. Some of the factors that determine this activity have been investigated. MATERIALS AND METHODS:Ferrocene-containing alcohols were tested for cytotoxicity against the HeLa cancer cell line. Cell survival was measured by means of the colorometric 3-(4,5-dimethylthiazol-2-yl)-diphenyltetrazolium bromide assay. RESULTS: The 50% lethal dosage of 4-ferrocenylbutanol was 5.72 micromol. dm(-3) and for 2-ferrocenylethanol and 3-ferrocenylpropanol it was 35.0 and 17 micromol. dm(-3) respectively while for ferrocenylmethanol IC50 was >100 micromol. dm(-3). CONCLUSION: A drug activity-structural relationship exists in that ferrocenyl drugs with longer side chains are more cytotoxic. Compounds with lower ferrocenyl group formal reduction potential are also more cytotoxic.