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Chemistry and biological activity of platinum (II) polyamines
Title
Chemistry and biological activity of platinum (II) polyamines.
Creator
Brenner, Dora Lynn., Florida Atlantic University, Louda, Deborah W., Carraher, Charles E.
Abstract/Description
One of the most common chemotherapeutic drugs in use today is cis-DDP. While this substance has been found useful in the treatment of various malignant neoplasias, it also has many adverse side effects. Recently, polymeric cis-DDP analogs have been prepared using potassium tetrachloroplatinate and various diamines. Testing of these polymeric analogs has shown that some are biologically active while others are biologically inactive. The goal of this research was to investigate the possible...
Show moreOne of the most common chemotherapeutic drugs in use today is cis-DDP. While this substance has been found useful in the treatment of various malignant neoplasias, it also has many adverse side effects. Recently, polymeric cis-DDP analogs have been prepared using potassium tetrachloroplatinate and various diamines. Testing of these polymeric analogs has shown that some are biologically active while others are biologically inactive. The goal of this research was to investigate the possible reasons for the differences in biological activity which had been observed. The biological activity of the diamine components, the molecular weight of the polymers, and the degradation of the polymers were examined to determine if any of these properties of the polymers could be correlated to their biological activities.
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Date Issued
1988
PURL
http://purl.flvc.org/fcla/dt/14469
Subject Headings
Polyamines--Physiological effect
Format
Document (PDF)
Cytokinetic effects of platinum (II) polyamines on three different cell lines using flow cytometry
Title
Cytokinetic effects of platinum (II) polyamines on three different cell lines using flow cytometry.
Creator
Fitch, Claire E., Florida Atlantic University, Hartmann, James X., Louda, Deborah W.
Abstract/Description
The association between cytotoxicity and cell cycle perturbation caused by cisplatin and two platinum (II) polyamines, containing a methotrexate or a 2-chloro-p-phenylenediamine component, was investigated in human ovarian carcinoma cells (CAOV3), murine Balb 3T3 fibroblasts and Chinese ovarian hamster cells by flow cytometric DNA/protein, DNA/RNA and DNA degradation assays. Continuous in vitro drug exposure caused a time- and dose-dependent suppression of growth. Flow cytometric analysis...
Show moreThe association between cytotoxicity and cell cycle perturbation caused by cisplatin and two platinum (II) polyamines, containing a methotrexate or a 2-chloro-p-phenylenediamine component, was investigated in human ovarian carcinoma cells (CAOV3), murine Balb 3T3 fibroblasts and Chinese ovarian hamster cells by flow cytometric DNA/protein, DNA/RNA and DNA degradation assays. Continuous in vitro drug exposure caused a time- and dose-dependent suppression of growth. Flow cytometric analysis revealed a multiplicity of cytokinetic perturbations, the most important of which was Go/G1 depletion and S phase arrest. The latter correlated with inhibition of DNA synthesis and subsequent inhibition of RNA and protein synthesis. Prolonged S phase arrest concomitant with DNA degradation, followed by RNA and protein degradation, resulted in cell death via apoptosis. The platinum polymers appear to be effective in vitro chemotherapeutic agents. The study of cytokinetic perturbations is useful in determining the relative potency of antitumor drugs and in monitoring drug effectiveness during treatment.
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Date Issued
1999
PURL
http://purl.flvc.org/fcla/dt/15626
Subject Headings
Cisplatin, Cell lines, Flow cytometry, Polymers
Format
Document (PDF)
Initial evaluation of organotin monomers and polymers as potential anticancer agents
Title
Initial evaluation of organotin monomers and polymers as potential anticancer agents.
Creator
Doucette, Randy D., Florida Atlantic University, Louda, Deborah W.
Abstract/Description
A large number of metal-containing compounds show significant activity against cancer cells and incorporating a metal into a polymer offers several possible advantages. Compounds of the type R2SnCl2 (R = methyl, ethyl, propyl, butyl, t-butyl, octyl and phenyl) were tested for the ability to inhibit the growth of Balb 3T3 mouse fibroblast cells and CAOV3 human ovarian carcinoma cells. Polymers of 2-chloro-1,4-benzenediamine and the same organotin dichloride were synthesized and tested as well....
Show moreA large number of metal-containing compounds show significant activity against cancer cells and incorporating a metal into a polymer offers several possible advantages. Compounds of the type R2SnCl2 (R = methyl, ethyl, propyl, butyl, t-butyl, octyl and phenyl) were tested for the ability to inhibit the growth of Balb 3T3 mouse fibroblast cells and CAOV3 human ovarian carcinoma cells. Polymers of 2-chloro-1,4-benzenediamine and the same organotin dichloride were synthesized and tested as well. For both monomers and polymers, the pattern of growth inhibition relative to the R group was butyl > propyl = t-butyl = octyl = phenyl > ethyl > methyl. This and other aspects of the structure-activity relationship of the monomers and polymers were examined.
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Date Issued
2006
PURL
http://purl.flvc.org/fcla/dt/13410
Subject Headings
Apoptosis--Molecular aspects, Polymeric composites, Organometallic compounds, Cancer--Molecular aspects, Antineoplastic agents--Testing, Polymers in medicine
Format
Document (PDF)
synthesis of chitosan-cis-DDP derivative
Title
The synthesis of chitosan-cis-DDP derivative.
Creator
Francis, Ann-Marie, Florida Atlantic University, Louda, Deborah W., Carraher, Charles E.
Abstract/Description
The formation of polymeric derivatives of the cancer drug Cis-dichlorodiaminoplatinum (II), cis-DDP, by the reaction of (1-4)-2-acetamide-2-deoxy-beta-D-glucose (Chitosan) with potassium tetrachloroplatinate is reported. Chelation of (1-4)-2-acetamide-2-deoxy-beta-D-glucose by tetrachloroplatinum (II) occurred through the amine groups leaving the hydroxyls unreacted and free to assist in making the products water soluble. It was hoped that such compounds would retain the anti tumor activity...
Show moreThe formation of polymeric derivatives of the cancer drug Cis-dichlorodiaminoplatinum (II), cis-DDP, by the reaction of (1-4)-2-acetamide-2-deoxy-beta-D-glucose (Chitosan) with potassium tetrachloroplatinate is reported. Chelation of (1-4)-2-acetamide-2-deoxy-beta-D-glucose by tetrachloroplatinum (II) occurred through the amine groups leaving the hydroxyls unreacted and free to assist in making the products water soluble. It was hoped that such compounds would retain the anti tumor activity of cis-DDP but produce fewer toxic side effects. Structural characterization involved infrared spectroscopy, mass spectroscopy, EDAX analytical methods. Products were also analyzed using light scattering photometry, elemental analysis and solubility studies. Additionally, the biological activity of water-soluble products was tested against selected cell lines.
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Date Issued
1999
PURL
http://purl.flvc.org/fcla/dt/15699
Subject Headings
Chitosan, Polymeric drugs
Format
Document (PDF)
SQER
Title
SQER.
Creator
Chamely-Wiik, Donna M., Haky, Jerome E., Louda, Deborah W., Romance, Nancy
Date Issued
2014-03-11
PURL
http://purl.flvc.org/fau/flvc_fau_islandoraimporter_10.1021_ed300689n_1521555360
Format
Citation