Antineoplastic activity of a series of ferrocene-containing alcohols.
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.


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).


CONCLUSIONS
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.
Shago
Rebotsamang F
RF
Department of Chemistry, University of the Free State, Bloemfontein, South Africa.
Swarts
Jannie C
JC
Kreft
Elke
E
Van Rensburg
Constance E J
CE
D000438:Alcohols / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D005296:Ferrous Compounds / Q000737:chemistry / Q000494:pharmacology*; D006367:HeLa Cells; D006801:Humans; D000075163:Metallocenes; D013329:Structure-Activity Relationship
D000438:Alcohols; D000970:Antineoplastic Agents; D005296:Ferrous Compounds; D000075163:Metallocenes; C004998:ferrocene