Abstract：
BACKGROUND:Oxidised ferrocenium compounds often possess antineoplastic activity. In contrast, reduced ferrocene derivatives frequently only show activity if cell components can oxidise them inside cells to the ferrocenium species. Ferrocene compounds having the lowest formal reduction potential are normally expected to be the most cytotoxic. Here we demonstrate this is not always the case. Some of the structure-related and physical properties that enhance ferrocenyl antineoplastic activity have been investigated. MATERIALS AND METHODS:Ferrocene-containing beta-diketones of the type FcCOCH2COR with Fc=ferrocenyl and R=CF3, CCl3, CH3, Ph(=C6H5, phenyl) and Fc, were tested for cytotoxicity against HeLa (human cervix epitheloid), COR L23 (human large cell lung carcinoma) and platinum resistant CoLo320DM (human colorectal) and COR L23/CPR cancer cell lines. Cell survival was measured by means of the colorometric 3-(4,5-dimethylthiazol-2-yl)-diphenyltetrazolium bromide (MTT) assay. RESULTS:The mean drug concentration from 3 experiments causing 50% cell growth inhibition, (IC50) values, varied between 4.5 and 85.0 micromol dm(-3'), with the CF3(-) containing beta-diketone being the most active. Drug activity was inversely proportional to the formal reduction potential, Eo', of the ferrocenyl group, and dependent on the R group in the general beta-diketone structure. The CF3 complex was more cytotocic than cisplatin inter alia against platinum-resistant cell lines, and at least eight times more reactive against cancer cell lines than against PHA (phytohaemagglutinin)-stimulated lymphocyte cultures. CONCLUSION:A drug activity-structural relationship exists in that ferrocenyl drugs with halogen substituents chains are more cytotoxic. Compounds with higher ferrocenyl group formal reduction potential and stronger acid strength (i.e. smaller pKa value) are more cytotoxic.
journal_name
Anticancer Resjournal_title
Anticancer researchauthors
Swarts JC,Vosloo TG,Cronje SJ,Du Plessis WC,Van Rensburg CE,Kreft E,Van Lier JEsubject
Has Abstractpub_date
2008-09-01 00:00:00pages
2781-4issue
5Aeissn
0250-7005issn
1791-7530journal_volume
28pub_type
杂志文章abstract：BACKGROUND:Despite the large use of bevabizumab in the treatment of primary tumors of the brain, there is only limited experience with brain metastases (BM) and no experience in the treatment of previously untreated secondary brain lesions. PATIENTS AND METHODS:We treated patients with BM, not suitable for local treat...
journal_title：Anticancer research
pub_type： 杂志文章
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更新日期：2013-09-01 00:00:00
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journal_title：Anticancer research
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journal_title：Anticancer research
pub_type： 杂志文章
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journal_title：Anticancer research
pub_type： 杂志文章
doi：10.21873/anticanres.14297
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journal_title：Anticancer research
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journal_title：Anticancer research
pub_type： 杂志文章
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journal_title：Anticancer research
pub_type： 杂志文章
doi：
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journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2004-05-01 00:00:00
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journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1998-01-01 00:00:00
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journal_title：Anticancer research
pub_type： 杂志文章
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journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2014-12-01 00:00:00
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journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2012-11-01 00:00:00
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journal_title：Anticancer research
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journal_title：Anticancer research
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doi：
更新日期：2011-09-01 00:00:00
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pub_type： 杂志文章
doi：
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doi：
更新日期：2012-05-01 00:00:00
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pub_type： 杂志文章
doi：10.21873/anticanres.11888
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journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2014-09-01 00:00:00
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journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2003-03-01 00:00:00
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journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2003-05-01 00:00:00
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journal_title：Anticancer research
pub_type： 杂志文章
doi：
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journal_title：Anticancer research
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更新日期：2008-03-01 00:00:00
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journal_title：Anticancer research
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doi：
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journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2014-10-01 00:00:00
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journal_title：Anticancer research
pub_type： 杂志文章,评审
doi：
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journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2010-01-01 00:00:00
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journal_title：Anticancer research
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doi：
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journal_title：Anticancer research
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