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...

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Veröffentlicht in:Anticancer research 2007-09, Vol.27 (5A), p.3431-3433
Hauptverfasser: SHAGO, Rebotsamang F, SWARTS, Jannie C, KREFT, Elke, VAN RENSBURG, Constance E. J
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container_end_page 3433
container_issue 5A
container_start_page 3431
container_title Anticancer research
container_volume 27
creator SHAGO, Rebotsamang F
SWARTS, Jannie C
KREFT, Elke
VAN RENSBURG, Constance E. J
description 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 μmol. dm -3 and for 2-ferrocenylethanol and 3-ferrocenylpropanol it was 35.0 and 17 μmol. dm -3 respectively while for ferrocenylmethanol IC 50 was >100 μmol. 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.
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J</creator><creatorcontrib>SHAGO, Rebotsamang F ; SWARTS, Jannie C ; KREFT, Elke ; VAN RENSBURG, Constance E. J</creatorcontrib><description>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 μmol. dm -3 and for 2-ferrocenylethanol and 3-ferrocenylpropanol it was 35.0 and 17 μmol. dm -3 respectively while for ferrocenylmethanol IC 50 was &gt;100 μmol. dm -3 . Conclusion: A drug activity-structural relationship exists in that ferrocenyl drugs with longer side chains are more cytotoxic. 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subjects Alcohols - chemistry
Alcohols - pharmacology
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Biological and medical sciences
Drug Screening Assays, Antitumor
Ferrous Compounds - chemistry
Ferrous Compounds - pharmacology
HeLa Cells
Humans
Medical sciences
Metallocenes
Structure-Activity Relationship
Tumors
title Antineoplastic Activity of a Series of Ferrocene-containing Alcohols
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