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Dissertations / Theses on the topic 'Antitumour'

Author: Grafiati

Published: 4 June 2021

Last updated: 25 July 2025

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1

Mokdsi, George. "Antitumour Metallocenes." Thesis, The University of Sydney, 2000. http://hdl.handle.net/2123/794.

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This thesis reports a study of the chemical stability and coordination chemistry of several antitumour metallocenes Cp2MCl2 (Cp = h5-C5H5; M = Ti 1, V 2, Nb 3, Mo 4), as well as derivatives of Cp2TiCl2 1, with nucleic acids, nucleic acid constituents and proteins. These studies were carried out in order to identify the biologically active species and more fully understand the molecular level mechanism of action of the antitumour metallocenes, in particular Cp2TiCl2 1, which is currently undergoing phase II clinical trials. The interactions of Cp2MoCl2 4 with four oligonucleotides were stud

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2

Mokdsi, George. "Antitumour Metallocenes." University of Sydney. Chemistry, 2000. http://hdl.handle.net/2123/794.

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This thesis reports a study of the chemical stability and coordination chemistry of several antitumour metallocenes Cp2MCl2 (Cp = h5-C5H5; M = Ti 1, V 2, Nb 3, Mo 4), as well as derivatives of Cp2TiCl2 1, with nucleic acids, nucleic acid constituents and proteins. These studies were carried out in order to identify the biologically active species and more fully understand the molecular level mechanism of action of the antitumour metallocenes, in particular Cp2TiCl2 1, which is currently undergoing phase II clinical trials. The interactions of Cp2MoCl2 4 with four oligonucleotides were stud

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3

Gate, Ernest N. "Investigations on new antitumour agents." Thesis, Aston University, 1985. http://publications.aston.ac.uk/12512/.

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4

Skelton, Lorraine Ann. "Pyridyl quinazolines as potential antitumour agents." Thesis, Institute of Cancer Research (University Of London), 1995. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.294789.

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5

Shi, Dong-Fang. "The medicinal chemistry of antitumour benzazoles." Thesis, University of Nottingham, 1995. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.283645.

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6

Langnel, David Antoine Fernand. "New synthetic routes to antitumour imidazotetrazines." Thesis, University of Nottingham, 2000. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.311742.

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7

Shahbakhti, Hassan. "Structure/activity relationships of antitumour diazridinylquinones." Thesis, University of Salford, 1996. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.308289.

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8

Ayuko, Washington O. "Free radicals as potential antitumour agents." Thesis, Aston University, 1991. http://publications.aston.ac.uk/12521/.

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The aim of this work was to use extremely low concentrations of free radical generating compounds as a 'catalyst' to trigger endogenous free radical chain reactions in the host and to selectively eliminate neoplastic cells in the host. To test the hypothesis, a number of free radical generating compounds were screened on several malignant cell lines in vitro to select model compounds that were used against tumour models in vivo. 2,2-Diphenyl-1-picrylhydrazyl (DPPH) and its derivatives were selected at the model compounds for in vivo experiments in view of their high cytotoxic potency against s

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9

Horspool, Keith R. "Structure-activity studies on antitumour imidazotetrazinones." Thesis, Aston University, 1988. http://publications.aston.ac.uk/12550/.

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10

Rafferty, Karen. "Novel organometallic compounds as potential antitumour agents." Thesis, University of Leeds, 2008. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.487773.

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11

Thompson, Andrew M. "Synthetic studies on a potential antitumour compound." Thesis, University of Canterbury. Chemistry, 1991. http://hdl.handle.net/10092/7832.

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Mycalamides A and B, isolated recently from a marine sponge of the genus Mycale, show strong in vitro and in vivo antiviral and antitumour properties. In this research, the chemistry of the mycalamides was explored and structure-activity relationships were determined, with the overall objective of producing analogues with better, or more selective biological activities. Along with this, the conformational behaviour of the mycalamides and a related compound, pederin, was examined. Simple esters, silyl and alkyl ethers of the hydroxyl and amide functionalities were prepared during initial studi

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12

Chew, Eng-Hui. "Development of antitumour quinols : a mechanistic approach." Thesis, University of Nottingham, 2005. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.430303.

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13

Wong, Pui Ee. "Novel aza-cyclic derivatives as antitumour agents." Thesis, University of Strathclyde, 2006. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.432099.

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14

Pass, M. "Synthesis of the antitumour antibiotic CC-1065." Thesis, Imperial College London, 1987. http://hdl.handle.net/10044/1/47592.

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15

Citossi, Francesca. "Self-assembling antitumour prodrugs for localised drug delivery." Thesis, University of Nottingham, 2016. http://eprints.nottingham.ac.uk/33345/.

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Localised cancer therapy is a developing strategy used to overcome the systemic toxicity associated with intravenous systemic chemotherapy, which still represents the primary route of administration for the majority of current anticancer agents. Low molecular weight gelators (LMWGs) have recently gained increasing popularity as drug delivery platforms for localised cancer therapy: they are small molecules, which self-assemble into a 3D network via non-covalent interactions. Due to their inherent biocompatibility, LMWGs represent a viable alternative to the extensively explored polymer based dr

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16

Flasz, Jakub Tadeusz. "Total synthesis of the antitumour natural product, (-)- echinosporin." Thesis, Queen's University Belfast, 2013. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.601477.

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The following dissertation describes a collection of results that led to a successful formal total synthesis of a naturally-occurring antitumour antibiotic, (-)..echinosporin. To achieve that, various synthetic strategies were developed and examined, all of which relied on a cycloadditive event as a key step to prepare the [3.4.0J-bicyclic framework of (-)-echinosporin. The synthesis was eventually accomplished using the Padwa [3+2] cycloaddition-elimination of allenylphenylsulphone to a chiral sugar enone 6 as a key transformation. it provided the first recorded example of this reaction used

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17

Nightingale, Karl. "DNA sequence recognition by the antitumour antibiotic bleomycin." Thesis, University of Southampton, 1992. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.241056.

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18

O'Sullivan, Noeleen. "Synthesis and reactions of cyclopropamitosenes and related pyrrolo[1,2-a]indoles." Thesis, Loughborough University, 1992. https://dspace.lboro.ac.uk/2134/14132.

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The use of Mitomycin C in the treatment of a wide range of neoplastic conditions is discussed. The mechanism of action of mitomycin anticancer antibiotics under reductive activation conditions using either enzymes, sodium dithionite, catalytic hydrogenation or chromium (Il) perchlorate is examined, as is the alkylation of DNA. An intramolecular [3+2] cycloaddition strategy has been employed to synthesise the pyrrolo[I,2-aJ]indole nucleus for a wide range of cyclopropamitosenes, whereas the key step in the synthesis of pyrrolo[I ,2-a]indoles without the cyclopropane ring was a modified Wittig r

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19

Spencer-Evans, Victoria Louise. "Design, synthesis and evaluation of linkers for the solid phase synthesis of pyrrolo [2,1-c][1,4] benzodiazepines." Thesis, University of Nottingham, 2003. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.289331.

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20

Trapini, Valentina. "The development of Phortress : from molecule to mechanism." Thesis, University of Nottingham, 2002. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.269467.

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21

Griffiths, Jonathan. "Structural modification of DNA." Thesis, University of Nottingham, 1991. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.315114.

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22

Robson, Claire. "Biochemical probes for folate-metabolising enzymes." Thesis, University of Newcastle Upon Tyne, 1994. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.240965.

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23

Jones, Garry B. "Design, synthesis and evaluation of DNA-binding oxazolo[2,3-c][1,4]benzodiazepines and pyrrolo[2,1-c][1,4]benzodiazepines." Thesis, University of Portsmouth, 1991. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.293269.

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24

Croker, Stephen John. "Synthetic studies towards a novel DNA targeted cross-linking agent based on DC-81 and CC-1065." Thesis, University of Portsmouth, 1997. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.310416.

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25

Murray, Clare Louise. "A new approach to the synthesis of DNA-interactive pyrrolo-[1,4]-benzodiazepin-5-ones." Thesis, University of Liverpool, 1996. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.321143.

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26

Fletcher, Michael Crawford. "Estimating the kinetic parameters of DNA sequence-selective drugs by footprinting." Thesis, University of Southampton, 1995. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.295695.

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27

Cui, Zong Jie. "Photodynamic drug action on rat pancreatic acinar cells." Thesis, University of Cambridge, 1989. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.306352.

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28

Cook, Richard Thomas. "Synthetic studies towards the sesbanimide group of antitumour agents." Thesis, University of Cambridge, 1987. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.329012.

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29

Gdarah, Khaled M. "The synthesis of some nucleoside analogues as antitumour agents." Thesis, Brunel University, 1993. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.332000.

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30

McCaig, Avril E. McCaig. "The synthesis of imidazole nucleosides as potential antitumour agents." Thesis, Heriot-Watt University, 1988. http://hdl.handle.net/10399/1989.

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31

Matthews, Charles S. "Investigations into the mechanism of action of antitumour quinols." Thesis, University of Nottingham, 2011. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.659198.

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Antitumour quinols containing the 4-hydroxycyclohexa-2,5-dienone pharmacophore potently inhibit human tumour cell growth in vitro and in vivo. This activity is postulated to occur via inhibition of the thioredoxin/thioredoxin reductase (TrxlTrxR) redox system which reduces numerous substrates involved in cellular proliferation, signal transduction, redox homeostasis and apoptosis. Similar to the archetypal quinol, PMX 464, its eventual successor, PMX 290, induced caspase-dependent apoptosis, cell cycle arrest and oxidative stress in sensitive tumour cells whilst depletion of glutathione increa

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32

Leong, Chee-Onn. "Antitumour benzothiazoles : analysis of DNA damage induced by Phortress." Thesis, University of Nottingham, 2003. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.396792.

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33

Stanslas, Johnson. "Mechanisms of the antitumour activities of novel polycyclic acridines." Thesis, University of Nottingham, 1998. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.263005.

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34

El-Sokkary, Ahmed Mohamed Adel. "The evaluation of new ruthenium complexes as antitumour agents." Thesis, University of Leeds, 2007. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.440638.

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35

Kadri, Hachemi. "Design, synthesis and biological evaluation of novel antitumour compounds." Thesis, Cardiff University, 2010. http://orca.cf.ac.uk/54364/.

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Cancer is a leading cause of death worldwide. Chemotherapy is the main approach used currently for the treatment and management of this disease especially disseminated malignant tumours. Traditional anticancer drugs have a limited selectivity as they target mainly DNA synthesis or cell proliferation leading to severe side effects. However, the newer anti-cancer drugs are more selective in targeting certain aberrant signalling pathways in cancer cells. In the first part of this work, a series of benzimidazole and indole analogues of a potent antitumour benzothiazole lead compound were synthesis

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36

George, Jonathan Harry. "Synthetic studies on the azinothricin family of antitumour antibiotics." Thesis, University College London (University of London), 2007. http://discovery.ucl.ac.uk/1446467/.

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A first synthesis of the acyl side chain of azinothricin and a second-generation route to the A83586C side chain is described in this thesis. The successful strategy was based on an asymmetric aldol reaction, a stereoselective Roush-type crotylboration and a Trost asymmetric allylic alkylation reaction to set the stereocentres of the key intermediates 3.95 and 3.5, which were subsequently coupled together to give the side chain fragment 3.105 after 10 further steps. The total synthesis of several A83586C/azinothricin analogues is also described. These hybrid structures have been formed via a c

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37

Clark, Alan S. "Antitumour imidazotetrazines: probes for the major groove of DNA." Thesis, Aston University, 1991. http://publications.aston.ac.uk/12602/.

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The antitumour imidazotetrazinones are believed to act as prodrugs for the triazene series of alkylating agents, showing a marked pteference for the alkylation of the middle guanine residue in a run of three or more contiguous guanines. However, the. exact nature of the interactions of imidazotetrazinones within the micro~environment of DNA are; as yet unknown. In order to examine such interactions a three pronged approach involving molecular modelling, synthetic chemistry and biological analysis has been undertaken during the course of this project. . Molecular modelling studies have shown th

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38

Deans, Bryan. "Studies on the mechanism of action on antitumour imidazotetrazinones." Thesis, Aston University, 1994. http://publications.aston.ac.uk/11048/.

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This thesis attempts to identify the cellular targets important to the cytotoxicity of imidazotetrazinones, to elucidate the pathways by which this damage leads to cell death, and to identify mechanisms by which tumour cells may circumvent this action. The levels of the DNA repair enzymes O6-alkylguanine-DNA-alkyltransferase (O6-AGAT) and 3-methyladenine-DNA-glycosylase (3MAG) have been examined in a range of murine and human cell lines with differential sensitivity to temozolomide. All the cell lines were proficient in 3MAG despite there being 40-fold difference in sensitivity to temozolomide

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39

Waern, Jenny Birgitta. "The biological chemistry of the antitumour agent molybdocene dichloride." Thesis, The University of Sydney, 2005. https://hdl.handle.net/2123/28105.

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This thesis reports a study of the coordination chemistry, cytotoxicity, and cellular uptake of molybdocene dichloride and a range of derivatives. These studies were performed to provide information about the mechanism of antitumour action and hence to evaluate the potential of molybdocene dichloride to proceed to clinical trials.

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40

Waring, M. A. "Studies related to chromenequinones." Thesis, University of Newcastle Upon Tyne, 1988. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.233290.

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41

O'Connor, P. M. "Crosslinking reactions of the dimethane sulphonates within chromatin." Thesis, University of Manchester, 1987. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.383233.

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42

Morris, Stephen James. "Design, synthesis and evaluation of a sequence-selective DNA cleaving agent based on the pyrrolo[2,1-c][1,4]benzodiazepine ring system : investigation of the DNA-reactive species." Thesis, University of Portsmouth, 1992. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.340240.

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43

Thompson, Stephen. "The synthesis of novel DNA-interactive pyrrolo-(2,1-c)[1,4]-benzodiazepin-5-ones." Thesis, University of Liverpool, 2000. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.367072.

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44

Holmes, Jennifer Jane. "Metabolism and mechanisms of action of novel pyrazoloacridone and anthraquinone cytotoxic agents." Thesis, University of Strathclyde, 1995. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.249821.

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45

Bull, Vincent L. "Studies on the mode of cytotoxicity of imidazotetrazinones." Thesis, Aston University, 1988. http://publications.aston.ac.uk/12506/.

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The irnidazotetrazinones are a novel group of anti tumour agents which have demonstrated good activity against a range of murine tumours and human xenografts. They possess a structure activity relationship similar to the anti tumour triazenes, with the chloroethyl (mitozolomide) and methyl (temozolomide) analogues being active antitumour agents, whilst the ethyl (CCRG 82019) and higher homologues are inactive. This thesiS attempts to elucidate the biological mechanisms responsible for the strict structure-activity relationship observed amongst the imidazotetrazinones. Mitozolomide is the only

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46

Chambers, Christopher Steven. "The synthesis of novel analogues of the antitumour antibiotic pyrrolobenzodiazepines." Thesis, University of Huddersfield, 2009. http://eprints.hud.ac.uk/id/eprint/7068/.

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In this thesis, the novel synthesis of tetra- and triazolo-analogues of the pyrrolobenzodiazepines, pyrrolobenzothiadiazepines, benzodiazepines and benzothiadiazepines are described. These compounds are of great interest as synthetic targets due to their potential medical properties. The key processes are the intramolecular 1,3-dipolar cycloaddition between the azide and the nitrile present in compound (1), the azide and the alkyne present in compound (2) the azide and the alkene present in compound (3), to form the novel final compounds of type (4). The synthesis of these precursors from read

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47

Kemp, Christopher Gary. "Total solid-phase sysnthesis of the mixrins : antitumour cyclic lipopeptides." Thesis, University College London (University of London), 2011. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.540430.

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48

Lazarides, Linos. "Synthetic studies on the A83586C/GE3 family of antitumour antibiotics." Thesis, University College London (University of London), 2005. http://discovery.ucl.ac.uk/1444925/.

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The A83586C/GE3 class of cyclodepsipeptides are a family of antitumour antibiotics whose antitumour properties have been attributed to their ability to inhibit E2F transcription factors. The latter are critical regulators of cellular proliferation that are potentially important new therapeutic targets for the control of proliferative diseases such as cancer. In this thesis, the asymmetric total synthesis of several A83586C/GE3/Verucopeptin analogues is described. Some of these molecules have provided valuable insights into the actual mechanism of antitumour activity for this class. All of thes

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49

Kerr, G. "The synthesis of pyrazole C-nucleosides as potential antitumour agents." Thesis, Heriot-Watt University, 1992. http://hdl.handle.net/10399/1454.

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50

Banks, Jason George. "Development of C8-linker chemistry for the pyrrolobenzodiazipine antitumour antibiotics." Thesis, University of Portsmouth, 1999. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.323324.

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