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Metabolic and biochemical studies on the anti-neoplastic agent, 5-(3,3-dimethy-1-triazeno)-imidazole-4-carboxamideBeal, Diane Dorothy. January 1977 (has links)
Thesis--Wisconsin. / Vita. Includes bibliographical references.
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Chemistry of 1,2-dialkynylimidazoles rearrangements to cyclopentapyrazines and imidazo[1,2-a]pyridines /Nadipuram, Asha Krishna, January 1900 (has links) (PDF)
Thesis (Ph. D.)--University of Texas at Austin, 2005. / Vita. Includes bibliographical references.
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The chemistry of aza-enediynes, aza-enyne allenes, and related aza-Bergman and aza-Myers-Saito rearrangementsFeng, Liping, January 1900 (has links) (PDF)
Thesis (Ph. D.)--University of Texas at Austin, 2005. / Vita. Includes bibliographical references.
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Biochemical and cytological effects of the anticancer alkaloid, acronycine, on tumor cells in cultureDunn, Bruce Partridge January 1974 (has links)
Acronycine is an acridone alkaloid occurring in the bark of the Australian scrub ash. It has been reported to have considerable anti-tumor activity against a variety of experimental neoplasms, and is currently undergoing clinical trials. Little is known of the mechanisms responsible for its antitumor activity. The current study describes some of the cytological and biochemical effects of the alkaloid on tumor cells in culture. The growth in vitro of L5I78Y mouse and IRC rat leukemia cells was inhibited by acronycine at concentrations of 3 to 12 μ the incorporation of extracellular nucleosides into intracellular nucleic acid precursor pools - this effect appeared to account entirely for the inhibition of the incorporation of these precursors into nucleic acids. The mechanism by which L5I78Y cells utilize extracellular uridine and by which acronycine interferes with this process were studied. The results of investigations into the kinetics and temperature dependence of uridine uptake by whole cells and of uridine phosphorylation by cell extracts suggested that: (i) the transport of uridine across the plasma membrane is a step independent from its subsequent phosphorylation, and (ii) this transport is normally rate-limiting in the uptake of this nucleoside. Acronycine, at concentrations which markedly inhibited uridine uptake in whole cells, had little or no effect on the phosphorylation of uridine in cell extracts. This and other evidence (including the effect of acronycine on the temperature dependence and kinetics of uridine uptake) suggested that the inhibition by acronycine of the utilization by L5I78Y cells of extracellular uridine results from an interference with the transport of the nucleoside across the plasma membrane. A similar mechanism may also account for the inhibition of the uptake of other nucleosides, as well as for a slight inhibition of choline and inositol uptake which was also observed in this study. 14C-acronycine was prepared and shown to be bound rapidly and reversibly to L5I78Y cells. It was also bound to non-dialysable serum components, in which form it appeared to no longer be available for interaction with cells. This latter effect may have implications for the us of acronycine in chemotherapy. Most or all of the observed effects of acronycine can tentatively be explained on the basis of a akaloid-induced alterations in membrane function. Acronycine is a relatively water-insoluble, lipophilic compound, and as such may reasonably be expected to interact with lipids and/or hydrophobic regions of proteins. It is speculated that interactions of this type with membrane components may be responsible for the biological effects of this compound. / Medicine, Faculty of / Biochemistry and Molecular Biology, Department of / Graduate
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Synthesis of protected amino thymidines and new thiol derivatives of the vascular targeting agent combretastatin A-4Ramirez, Daniel A. Kane, Robert R. January 2006 (has links)
Thesis (M.S.)--Baylor University, 2006. / Includes bibliographical references (p. 63-65).
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Screening of natural products and alkylating agents for antineoplastic activityKanyanda Stonard Sofiel Elisa January 2007 (has links)
<p><b><font face="TimesNewRomanPS-BoldMT">
<p align="left">Apoptosis is a process in which a cell programmes its own death. It is a highly organized physiological mechanism in which injured or damaged cells are destroyed. Apart from physiological stimuli however, exogenous factors can induce apoptosis. Many anti-cancer drugs work by activating apoptosis in cancer cells. Natural substances have been found to have the ability to induce apoptosis in various tumour cells and these substances have been used as templates for the construction of novel lead compounds in anticancer treatment. On the other hand, alkylating agents such as cisplatin, cis- [PtCl2 (NH3) 2]have been widely used as antineoplastic agents for a wide variety of cancers including testicular, ovarian, neck and head cancers, amongst others. However, the use of cisplatin as an anticancer agent is limited due to toxicity and resistance problems. <font face="TimesNewRomanPSMT">The aim of this present study was to screen the leaves of </font><i><font face="TimesNewRomanPS-ItalicMT">Rhus laevigata</font><font face="TimesNewRomanPSMT">, a South African indigenous plant, for the presence of pro-apoptotic and anti-proliferative natural compounds and also to screen newly synthesised palladium based complexes (15 and 57) and a platinum based complex (58) for their antineoplastic activities tested against a panel of cell lines.</font></i></p>
</font><font face="TimesNewRomanPS-BoldMT">
<p align="left">  / </p>
</font></b></p>
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Screening of natural products and alkylating agents for antineoplastic activityKanyanda Stonard Sofiel Elisa January 2007 (has links)
<p><b><font face="TimesNewRomanPS-BoldMT">
<p align="left">Apoptosis is a process in which a cell programmes its own death. It is a highly organized physiological mechanism in which injured or damaged cells are destroyed. Apart from physiological stimuli however, exogenous factors can induce apoptosis. Many anti-cancer drugs work by activating apoptosis in cancer cells. Natural substances have been found to have the ability to induce apoptosis in various tumour cells and these substances have been used as templates for the construction of novel lead compounds in anticancer treatment. On the other hand, alkylating agents such as cisplatin, cis- [PtCl2 (NH3) 2]have been widely used as antineoplastic agents for a wide variety of cancers including testicular, ovarian, neck and head cancers, amongst others. However, the use of cisplatin as an anticancer agent is limited due to toxicity and resistance problems. <font face="TimesNewRomanPSMT">The aim of this present study was to screen the leaves of </font><i><font face="TimesNewRomanPS-ItalicMT">Rhus laevigata</font><font face="TimesNewRomanPSMT">, a South African indigenous plant, for the presence of pro-apoptotic and anti-proliferative natural compounds and also to screen newly synthesised palladium based complexes (15 and 57) and a platinum based complex (58) for their antineoplastic activities tested against a panel of cell lines.</font></i></p>
</font><font face="TimesNewRomanPS-BoldMT">
<p align="left">  / </p>
</font></b></p>
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Study on the in vitro anti-tumor effect of Acanthopanax senticosus.January 2008 (has links)
Wan, Chung Tin. / Thesis (M.Phil.)--Chinese University of Hong Kong, 2008. / Includes bibliographical references (leaves 126-139). / Abstracts in English and Chinese. / Thesis / Assessment Committee --- p.i / Acknowledgement --- p.ii / Abstract (English) --- p.iii / Abstract (Chinese) --- p.v / List of Abbreviations --- p.vii / List of Tables --- p.ix / List of Figures --- p.x / Chapter Chanter 1 --- Introduction / Chapter 1.1. --- Overview of cancer --- p.1 / Chapter 1.1.1 --- Breast cancer --- p.1 / Chapter 1.1.2 --- Hepatocellular carcinoma (HCC) --- p.2 / Chapter 1.2. --- Role of natural products in the fight against cancer --- p.3 / Chapter 1.2.1 --- Introduction of Astragalus membranaceus --- p.4 / Chapter 1.2.2 --- Introduction of Acanthopanax senticosus --- p.9 / Chapter 1.2.3 --- Introduction of Grifola Frondosa --- p.13 / Chapter 1.3. --- Apoptosis and cancer --- p.17 / Chapter 1.3.1 --- Caspases --- p.20 / Chapter 1.3.2 --- Intrinsic apoptotic pathway --- p.21 / Chapter 1.3.3 --- Extrinsic apoptotic pathway --- p.23 / Chapter 1.3.4 --- Execution of apoptosis --- p.26 / Chapter 1.4 --- Cell cycle and cancer --- p.27 / Chapter 1.5 --- Objective of this project: --- p.29 / Chapter Chapter 2 --- Materials and Methods / Chapter 2.1 --- Materials: --- p.30 / Chapter 2.1.1 --- Culture medium --- p.30 / Chapter 2.1.2 --- Buffers and reagents --- p.31 / Chapter 2.1.3 --- Herbs --- p.34 / Chapter 2.2 --- Methods --- p.35 / Chapter 2.2.1 --- Cell cultures --- p.35 / Chapter 2.2.1.1 --- Cell lines --- p.35 / Chapter 2.2.1.2 --- Cell culture techniques --- p.36 / Chapter 2.2.1.3 --- Cryopreservation of cell lines --- p.36 / Chapter 2.2.2 --- Proliferation assay --- p.37 / Chapter 2.2.2.1 --- MTT assay --- p.37 / Chapter 2.2.2.2 --- Isolation of PBMC --- p.38 / Chapter 2.2.2.3 --- XTT --- p.39 / Chapter 2.2.3 --- DNA fragmentation --- p.39 / Chapter 2.2.4 --- Flow cytometry --- p.41 / Chapter 2.2.4.1 --- Detection of mitochondrial membrane depolarization by the use of JC-1 --- p.41 / Chapter 2.2.4.2 --- Annexin-V-FITC PI labeling of apoptotic cells --- p.42 / Chapter 2.2.4.3 --- Cell cycle analysis --- p.43 / Chapter 2.2.5 --- Western blotting --- p.43 / Chapter 2.2.5.1 --- Total protein extraction --- p.44 / Chapter 2.2.5.2 --- Determining protein concentration --- p.44 / Chapter 2.2.5.3 --- SDS-PAGE --- p.45 / Chapter 2.2.5.4 --- Electroblotting --- p.45 / Chapter 2.2.5.5 --- Probing --- p.46 / Chapter 2.2.5.6 --- ECL --- p.46 / Chapter 2.2.6 --- Preparation of herbal extracts --- p.47 / Chapter 2.2.6.1 --- Preparation of extract of Astragalus membranaceus and Grifola frondosa --- p.47 / Chapter 2.2.6.2 --- Preparation of Acanthopanax senticosus aqueous extract --- p.47 / Chapter 2.2.6.3 --- Partition of Acanthopanax --- p.47 / Chapter 2.2.6.4 --- Column purification of ethyl-acetate fraction --- p.48 / Chapter 2.2.6.5 --- Analytical thin layer chromatography --- p.49 / Chapter 2.2.7 --- Statistical Analysis --- p.50 / Chapter Chanter 3 --- Results / Chapter 3.1 --- Extractions --- p.51 / Chapter 3.2 --- Anti-proliferative effect of herbal extracts on cancer cell lines --- p.51 / Chapter 3.3 --- Partition of Acanthopanax methanol extract --- p.56 / Chapter 3.4 --- Anti-proliferative effect of Acanthopanax partition fractions on breast cancer cells --- p.59 / Chapter 3.5 --- Column chromatography of ethyl acetate fraction --- p.59 / Chapter 3.6 --- Anti-proliferative effect of various sub-fractions on breast cancer cells --- p.64 / Chapter 3.7 --- Effect of sub-fractions on PBMC proliferation --- p.76 / Chapter 3.8 --- Kinetic study of anti-proliferative effect of Fc --- p.76 / Chapter 3.9 --- Flow cytometric analysis --- p.79 / Chapter 3.91 --- JC-1 staining --- p.79 / Chapter 3.92 --- Annexin-P1 labeling --- p.79 / Chapter 3.93 --- Cell cycle analysis --- p.80 / Chapter 3.10 --- DNA fragmentation assay --- p.88 / Chapter 3.11 --- Western blotting --- p.91 / Chapter Chanter 4 --- Discussion --- p.99 / Chapter Chapter 5 --- Conclusion --- p.124 / References --- p.126
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Investigations into the chemical mechanisms of biological activity by heterocyclic di-N-oxides and 1,2 benzodithiolan-3-one 1-oxides /Ganley, Brian Christopher, January 2000 (has links)
Thesis (Ph. D.)--University of Missouri--Columbia, 2000. / "December 2000." Typescript. Vita. Includes bibliographical references. Also available on the Internet.
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Design and biological evaluation of novel antitumor agents with mechanisms of action against topoisomerase II and/or G-quadruplexesKim, Mu-yong 28 August 2008 (has links)
Not available / text
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