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  • 1
    Electronic Resource
    Electronic Resource
    A Preliminary Study of the Toxicological Properties of Selected Polymer–Ferrocene Conjugates (2000)
    Springer
    Journal of inorganic and organometallic polymers and materials 10 (2000), S. 177-188 
    Details
    ISSN: 1572-8870
    Keywords: toxicology ; polymer–ferrocene conjugates ; polymer–platinum conjugates ; cisplatin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Prompted by early observations of the cytotoxic and antineoplastic properties of certain ferrocene and ferricenium derivatives, efforts in this laboratory were focused on the synthesis of carrier-bound ferrocene compounds. Subsequent cell culture tests carried out with selected conjugates obtained in that program showed these polymers to be highly active antiproliferative agents. In the present project toxicological work has been performed in vivo on several ferrocene conjugates in an effort to assess their toxic effects in experimental animals (CD-1 mice). The conjugates, all based on an α,β-DL-polyaspartamide backbone structure, comprise the ferrocene drug model as a terminal on short side chains containing biofissionable amide or ester links for intracellular drug release. The polymers, dissolved in phosphate-buffered saline, have been injected in predetermined concentrations into the vein of the mice, and the maximum tolerated dose (MTD) levels have been determined, the latter referring to the highest dose levels administered that would allow long-term survival of the test animals. For the five conjugates tested, MTD levels range from about 3 to 30 mg Fe/kg or 0.05–0.66 mmol Fe/kg. Compared on a molar metal-to-metal basis with similarly structured platinum conjugates tested previously (MTD, ∼0.14–2.66 mmol Pt/kg), these values are indicative of comparatively high toxicity of the ferrocene polymers. Some implications of these findings are discussed.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1016686522012
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  • 2
    Electronic Resource
    Electronic Resource
    Antiproliferative Activity of Polymer-Bound, Monoamine-Coordinated Platinum Complexes Against LNCaP Human Metastatic Prostate Adenocarcinoma Cells (2000)
    Springer
    Journal of inorganic and organometallic polymers and materials 10 (2000), S. 51-60 
    Details
    ISSN: 1572-8870
    Keywords: antiproliferative activity ; water-soluble polymer–platinum complexes ; LNCaP human metastatic prostate adenocarcinoma
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The chemotherapeutic treatment of secondary, i.e., disseminated cancers, has until now remained an unsatisfactory modality. The LNCaP human metastatic prostate adenocarcinoma cell line lends itself as a useful tool to probe the efficaciousness of novel antineoplastic agents for the control of metastatic cell growth. In this paper we report on a series of cell culture tests assessing the antiproliferative activity of several water-soluble polymer–platinum conjugates in which the metal is tied (anchored) to various polymeric carriers through coordination by a single carrier-attached primary amine ligand. The conjugates are based on polyaspartamide carriers composed, within the backbone, of a majority fraction of subunits bearing water-solubilizing tertiary amine side-group functions and a minority fraction of subunits featuring side chain-terminating primary amino groups for metal binding. Two similarly structured conjugates in which the platinum center is coordinated by two amine ligands in cisoid orientation mimicking the structural skeleton of cisplatin are included in the study for comparison. In all structures cleavage of a side-chain segment is required for release of the monomeric bioactive platinum complex. The growth of LNCaP human metastatic prostate adenocarcinoma cells in RPMI 1640 medium in the presence and absence of the conjugates in a range of concentrations is assessed by a protein assay, and the IC50 values, representing the drug concentrations required for 50% cell growth inhibition relative to untreated control, are determined. The results show both classes of conjugates, those comprising monoamine-coordinated platinum and those featuring cis-diamine-coordinated metal, to be well comparable in antiproliferative activity. A major program of synthesis and evaluation of polymer-bound monoamineplatinum complexes, prompted by these findings, is forthcoming in this laboratory.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1009456532763
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  • 3
    Electronic Resource
    Electronic Resource
    Antiproliferative Activity of Polyaspartamide–Ferrocene Conjugates Containing the Biofissionable Carboxamide Function in the Anchoring Links (2000)
    Springer
    Journal of inorganic and organometallic polymers and materials 10 (2000), S. 93-101 
    Details
    ISSN: 1572-8870
    Keywords: ferrocene polymers ; polyaspartamide carriers ; carboxamide ; LNCaP cell line
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract In continuation of earlier studies probing the cytotoxic properties of polymer-bound ferrocene against the HeLa cell line, the present communication presents the results of cell culture tests performed on a number of polymer–ferrocene conjugates against the LNCaP human metastatic prostate adenocarcinoma line. The water-soluble substrates are polyaspartamide carriers containing primary amine functions as side-group terminals to which the ferrocenylation agent, 4-ferrocenylbutanoic acid, is covalently bound (anchored) through N-acylation, the carboxamide groups so generated in the tether acting as the biofissionable links for release of the monomeric ferrocene compound from the conjugate in the lysosomal compartment. The carrier backbone structures are of the α, β-DL-peptide type preferred in our ongoing work, as this structural configuration allows ultimate chain degradation for efficacious excretion yet prevents fast and premature, α-peptidase-mediated “unzipping” of the peptidic chain. The screens are performed by exposing the selected conjugates 1–7 at various concentrations to cultured LNCaP cells in RPMI medium over a period of 7 days and assessing cell viability by a protein assay. From cell growth data relative to control, plotted against conjugate concentration, the IC50 values, expressed as metal concentrations required for 50% cell growth inhibition, are found to be in the narrow range of 1–10 μg Fe/ml. This compares well with earlier results obtained on selected ferrocene conjugates against the HeLa cell line and, more strikingly still, on analogous, previously tested conjugates containing the square-planar structural skeleton of the cisplatin-type anticancer drug system as the bioactive agent. The present findings, hence, should provide a healthy motivation for more extended studies of polymer-anchored ferrocenes in the biomedical realm.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1009475909111
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    Paper (German National Licenses)
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