title: Antineoplastic activity of a series of ferrocene-containing alcohols.
abstract: 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.
authors.affiliation: Department of Chemistry, University of the Free State, Bloemfontein, South Africa.
authors.forename: Rebotsamang F
authors.initials: RF
authors.lastname: Shago
authors.forename: Jannie C
authors.initials: JC
authors.lastname: Swarts
authors.forename: Elke
authors.initials: E
authors.lastname: Kreft
authors.forename: Constance E J
authors.initials: CE
authors.lastname: Van Rensburg
mesh_terms: 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
chemical_list: D000438:Alcohols; D000970:Antineoplastic Agents; D005296:Ferrous Compounds; D000075163:Metallocenes; C004998:ferrocene