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Dissertations / Theses on the topic 'DNA Binding Anticancer Drugs'

Author: Grafiati

Published: 4 June 2021

Last updated: 7 September 2023

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1

Leczkowska, Anna. "Non-covalent DNA-binding ruthenium anticancer drugs." Thesis, University of Birmingham, 2011. http://etheses.bham.ac.uk//id/eprint/1695/.

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The research work described in this thesis concerns metal-based anticancer drugs with an emphasis on non-covalent DNA-binding supramolecular assemblies. The project involves the preparation of a series of mono- and bi-metallic ruthenium complexes with a primary focus on fluorescent dinuclear triple-stranded helicates with different structural topographies. Emphasis is then directed towards an investigation of the DNA binding characteristics of these molecules and an evaluation of their anticancer properties in human cancer cell lines. Attention is brought to the significance that the cylinder-

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2

Todd, Ryan Christopher 1981. "Structural and functional consequences of platinum anticancer drug binding to free and nucleosomal DNA." Thesis, Massachusetts Institute of Technology, 2010. http://hdl.handle.net/1721.1/57802.

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Thesis (Ph. D.)--Massachusetts Institute of Technology, Dept. of Chemistry, 2010.<br>Vita. Cataloged from PDF version of thesis.<br>Includes bibliographical references.<br>Cisplatin, carboplatin, and oxaliplatin are three FDA-approved members of the platinum anticancer drug family. These compounds induce apoptosis in tumor cells by binding to nuclear DNA, forming a variety of adducts, and triggering cellular responses, one of which is the inhibition of transcription. The focus of this thesis is on studying the structure of these adducts, and correlating these effects with inhibition of transcr

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3

Farhad, Mohammad. "Studies on new trinuclear palladium compounds." Connect to full text, 2007. http://hdl.handle.net/2123/2477.

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Doctor of Philosophy(PhD)<br>The present study deals with the synthesis and characterization of six tri-palladium complexes code named MH3, MH4, MH5, MH6, MH7 and MH8 that contained two planaramine ligands bound to the central or each of the terminal metal ions. The activity of the compounds against human cancer cell lines: A2780, A2780cisR and A2780ZD0473R, cell uptake, levels of DNA-binding and nature of interaction with salmon sperm and pBR322 plasmid DNA have also been determined. Whereas cisplatin binds with DNA forming mainly intrastrand GG adduct that causes local bending of a DNA stran

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4

Majmudar, Pooja M. "Investigating Molecular Targets of Phosphaplatins: A Class of Novel Non-DNA-Binding Platinum Anticancer Agents in the Treatment of Ovarian Cancer." Ohio University / OhioLINK, 2011. http://rave.ohiolink.edu/etdc/view?acc_num=ohiou1300373466.

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5

Trimmer, Elizabeth Eloise 1966. "Specific binding of human SRY (Sex-Determining Region Y) to DNA adducts of the anticancer drug cisplatin." Thesis, Massachusetts Institute of Technology, 1997. http://hdl.handle.net/1721.1/46076.

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6

Hotze, Anna Catharina Genovefa. "Design of ruthenium anticancer drugs : study of the structure-activity relationships and binding to DNA model bases of ruthenium complexes with 2-phenylazopyridine ligands /." Rotterdam : Optima Grafische Communicatie, 2003. http://catalogue.bnf.fr/ark:/12148/cb399315937.

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7

Bezoski, Brittany A. "Metal Binding Characteristics of Heterocyclic and Carbocyclic Anticancer Drugs." University of Toledo Health Science Campus / OhioLINK, 2016. http://rave.ohiolink.edu/etdc/view?acc_num=mco1481287656969232.

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8

Punchihewa, Chandanamalie. "DNA and DNA-Interacting Proteins as Anticancer Drug Targets." Diss., The University of Arizona, 2006. http://hdl.handle.net/10150/194379.

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DNA is both the oldest and newest of targets for cancer therapy. While it is already being targeted by many anticancer drugs in the clinic, the development of sequence-specific DNA binders has brought it back to the limelight as a valuable anticancer drug target.My studies on DNA interacting agents was initiated with the DNA intercalator campotothecin, and also included topoisomerase I enzyme. I have evaluated the structure of topoisomerase I C-terminal domain that consists of the active site tyrosine. My data indicate that this domain exists in a molten globule conformation with a fluctuating

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9

Jung, Yongwon 1977. "Cellular responses against DNA damaged by platinum anticancer drugs." Thesis, Massachusetts Institute of Technology, 2005. http://hdl.handle.net/1721.1/33746.

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Thesis (Ph. D.)--Massachusetts Institute of Technology, Dept. of Chemistry, 2005.<br>Vita.<br>Includes bibliographical references.<br>The anticancer activity of platinum-based drugs such as cisplatin, carboplatin, and oxaliplatin is mediated by their ability to attack DNA such that generated adducts trigger numerous cellular responses. A better understanding of these processes is critical for developing more effective therapeutic approaches, which can increase the anti-cancer activity of the drugs while minimizing side effects and extending successful treatment to a wider range of human cancer

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10

Sobhanian, Ali. "Synthetic and spectral studies of potential anticancer drugs." Thesis, University of Hertfordshire, 1997. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.361263.

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11

Ward, T. H. "Bioreductive anticancer drugs : a comet study on mechanisms and DNA damage." Thesis, University of Salford, 1998. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.245022.

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12

Matkar, Smita S. "Mechanism of action of potential anticancer drugs." Scholarly Commons, 2008. https://scholarlycommons.pacific.edu/uop_etds/2368.

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Traditionally, inoperable or metastatic cancers have been treated by causing massive DNA damage in order to induce self-destruction (apoptosis) of the rapidly multiplying cancer cells. Initially, this strategy works for many cancers, in particular those which express normal p53 tumor suppressor protein. However, most cancers eventually aquire mutations in either p53 or other signaling molecules and fail to initiate apoptosis in response to severe DNA damage. During this study three types of compounds were investigated for their DNA damaging and anticancer effects: a pair of novel metal contain

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13

Munnur, Deeksha Ganesh. "Structural studies of DNA complexes with minor groove-binding drugs." Thesis, University College London (University of London), 2012. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.550498.

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Targeting the minor groove of DNA with small molecules is an important recognition strategy in biology. A wide range of minor groove binding ligands (MGBLs) with good sequence discrimination ability are of interest as potential therapeutic agents in a variety of human diseases such as cancer, along with anti-bacterial and/or anti-parasitic activities. Whilst the detailed mechanism of action of some of these MGBLs is still unproven, they are known to be effective inhibitors of a number of minor and major groove binding protein-DNA interactions. This thesis reports on crystallographic studies to

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14

Ellis, T. "Controlled manipulation of gene expression with sequence-selective DNA-binding drugs." Thesis, University of Cambridge, 2004. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.598822.

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Three sets of synthetic DNA-binding drugs have been evaluated, largely by DNase I footprinting, to determine their affinity and selectivity for DNA sequences. MOLRAC bis-intercalator compounds produced by novel synthesis were found to be relatively insoluble with low affinity for DNA and little sequence-selectivity. Pyrrolobenzodiazepine (PBD) conjugates designed to bind covalently to DNA were shown to have reasonable affinity for DNA and moderate sequence-selectivity. Bacterial <i>in vitro</i> transcription assays demonstrated that covalent linkage to DNA could selectively block transcription

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15

Martin, Christopher Roland Hopker. "Modification of gene expression by small sequence-selective DNA-binding drugs." Thesis, University of Cambridge, 2005. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.615096.

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16

Celik, Haydar. "Enzyme-catalyzed Reductive Activation Of Anticancer Drugs Idarubicin And Mitomycin C." Phd thesis, METU, 2008. http://etd.lib.metu.edu.tr/upload/3/12609247/index.pdf.

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Idarubicin (IDA) and mitomycin C (MC) are clinically effective quinone-containing anticancer agents used in the treatment of several human cancers. Quinone-containing anticancer drugs have the potential to undergo bioreduction by oxidoreductases to reactive species, and thereby exert their cytotoxic effects. In the present study, we investigated, for the first time, the potential of IDA, in comparison to MC, to undergo reductive activation by NADPH-cytochrome P450 reductase (P450R), NADH-cytochrome b5 reductase (b5R) and P450R-cytochrome P4502B4 (CYP2B4) system by performing both in vitro plas

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17

Berndtsson, Maria. "On the role of different signal transduction pathways in induction of apoptosis by anticancer drugs /." Stockholm, 2007. http://diss.kib.ki.se/2007/978-91-7357-176-0/.

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18

Sprague, Robin M. "Molecular modeling of DNA with minor groove binding agents and intercalators." Scholarly Commons, 2000. https://scholarlycommons.pacific.edu/uop_etds/539.

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The molecular modeling of several drugs in complexes with deoxyribonucleic acid (DNA) was undet1aken. Selected bis-lexitropsins, based upon NMR and modeling studies of bis-distamycin A, were modeled with an oligonucleotide d(CGAACA TGTTCG)2 using MidasPlus and AMBER 4.0. Intercalators ethidium, ellipticinc. mitoxantrone, and bisantrene were modeled with an oligonucleotide d(CGCG)~ using SpartanPlus and DOCK 4.0. The binding site was prepared from an x-ray study of this oligonucleotide interacting with ditercalinium, a bis-intercalator. The purpost: of this study was to estimate the conformatio

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19

Shi, Ke. "X-ray crystallographic studies on Oligonucleotide structures and their complexes with intercalating and minor groove binding anticancer drugs /." The Ohio State University, 1999. http://rave.ohiolink.edu/etdc/view?acc_num=osu1488190109869963.

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20

Moniodis, Joseph John. "Studying the DNA binding of a non-covalent analogue of the trinuclear platinum anticancer agent BBR3464." University of Western Australia. School of Biomedical, Biomolecular and Chemical Sciences, 2006. http://theses.library.uwa.edu.au/adt-WU2007.0008.

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[Truncated abstract] The Phase II clinical candidate, [(trans-Pt(NH3)2Cl)2{μ-trans-Pt(NH3)2(H2N(CH2)6NH2)2}]4+ (BBR3464 or 1,0,1/t,t,t) shows a unique binding profile when compared to the anticancer agent cis-[Pt(NH3)2Cl2] (cisplatin) and dinuclear platinum complexes of the general formula [(trans-Pt(NH3)2Cl)2(H2N(CH2)nNH2)]2+. There is evidence that the increased efficacy of 1,0,1/t,t,t results from the presence of the charged central linker, which can alter the mode of binding to DNA. This alternate binding mode may be due to an electrostatic and hydrogen bonding association of the central p

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21

Smith, Kayleigh Ann. "The potential role of TOP2B in therapy-related leukaemia." Thesis, University of Newcastle Upon Tyne, 2012. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.627728.

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22

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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23

Jarvis, Ian William Harry. "Investigation of DNA adducts formed in cells and clinical tumour biopsies following exposure to platinum-containing anticancer drugs." Thesis, University of Newcastle Upon Tyne, 2011. http://hdl.handle.net/10443/1082.

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Platinum-based anticancer drugs are believed to exert their action through chemical reactions with genomic DNA, forming adducts with DNA bases. Although the pharmacology of such adducts has been widely studied, the cytotoxic mechanism remains unclear. The possibility that non-DNA molecules have the potential to alter the types of adducts formed has received very little attention, and limited information is available on the levels of adducts formed in clinical tumours. Further understanding of platinum-DNA adduct formation may be important in explaining the efficacy of platinum-based drugs in d

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24

Chhouri, Houssein. "Analysis by DNA barcoding of the heterogeneous response to anticancer drugs by different subpopulations of lung cancer cells." Electronic Thesis or Diss., Normandie, 2022. http://www.theses.fr/2022NORMR037.

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Le cancer est une maladie évolutive, caractérisée par l’existence d’un mélange complexe de plusieurs sous-populations cellulaires qui peuvent évoluer en réponse aux conditions environnementales. Cette hétérogénéité intratumorale a des conséquences extrêmement importantes, non seulement sur la progression tumorale, les métastases, mais aussi sur l’efficacité des traitements. Le cancer bronchique non à petites cellules (CBNPC) avec mutations activatrices de l’Epidermal Growth Factor Receptor (EGFR) est traité avec des inhibiteurs spécifiques de ce récepteur. Malheureusement, après une réponse fa

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25

Camp, Claire L. "Combining elemental and molecular mass spectrometry to study 3 types of biologically important compounds : DNA, phosphopeptides and anticancer drugs." Thesis, Loughborough University, 2014. https://dspace.lboro.ac.uk/2134/15129.

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Mass spectrometry was used to investigate three important biological molecules, deoxyribonucleic acid (DNA), phosphopeptides and oxaliplatin. The quantification of DNA is traditionally performed by UV spectroscopy; however the results can be affected greatly by the sample matrix. The method developed quantified phosphorus in digested calf thymus DNA and human DNA by high performance liquid chromatography (HPLC) coupled to inductively coupled plasma mass spectrometry (ICP-MS). The method presented showed excellent baseline separation between all 4 DNA mono-nucleotides and 5 UMP. Column recoveri

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26

Leslie, Kristofer David. "The interaction of sequence-specific ligands with the nucleosome." Thesis, University of Southampton, 2001. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.367975.

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27

Basili, Serena. "Computational Approaches for the Rational Design of Novel Topoisomerase I Poisons as Potential Anticancer Drugs." Doctoral thesis, Università degli studi di Padova, 2009. http://hdl.handle.net/11577/3426128.

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Topoisomerase I (TopoI) is an essential DNA-targeting enzyme which alters the supercoiling of DNA through a concerted process of breaking and rejoining of a DNA strand, thereby controlling the DNA topology required for replication and transcription. TopoI mediates relaxation of supercoiled DNA by creating a transient single-strand break in the DNA duplex that originates from a transesterification reaction involving a nucleophilic attack by the active-site tyrosine (Tyr723) hydroxyl group on a DNA phosphodiester bond situated at the site of cleavage. The resulting 3'-phosphotyrosine enzyme-DNA

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28

Sprague, Robin M. "Molecular modeling of DNA with minor groove binding agents and intercalators : a thesis." Scholarly Commons, 2001. https://scholarlycommons.pacific.edu/uop_etds/539.

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The molecular modeling of several drugs in complexes with deoxyribonucleic acid (DNA) was undet1aken. Selected bis-lexitropsins, based upon NMR and modeling studies of bis-distamycin A, were modeled with an oligonucleotide d(CGAACA TGTTCG)2 using MidasPlus and AMBER 4.0. Intercalators ethidium, ellipticinc. mitoxantrone, and bisantrene were modeled with an oligonucleotide d(CGCG)~ using SpartanPlus and DOCK 4.0. The binding site was prepared from an x-ray study of this oligonucleotide interacting with ditercalinium, a bis-intercalator. The purpost: of this study was to estimate the conformatio

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29

Sabatino, Maria Antonietta. "Combination treatments in in vitro and in vivo models between molecules reverting epigenetic gene silencing and DNA-interacting anticancer drugs." Thesis, Open University, 2008. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.502390.

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Epigenetic transcriptional gene silencing plays a fundamental role in cancer development and has been considered as a target for cancer therapy in the last few years, mainly due to its reversibility by small molecules. Among the several methylated genes investigated, glutathione-S-transferase CGST) PI, a protein belonging to cellular detoxification systems, has been shown to be extensively promoter-methylated in prostate cancer. My study therefore describes a new therapeutic approach against prostate cancer, based on the combination of demethylating agents and brostallicin, a DNA minor groove

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30

Ruhayel, Rasha A. "Multinuclear platinum anticancer therapeutics : insights into their solution chemistry and DNA binding interactions from NMR spectroscopy and molecular modelling." University of Western Australia. School of Biomedical, Biomolecular and Chemical Sciences, 2010. http://theses.library.uwa.edu.au/adt-WU2010.0021.

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In the 1980's, Nicholas Farrell developed a range of structurally distinct multinuclear Pt complexes that form long-range interstrand crosslinks (IXLs) in DNA. The dinuclear complex [{trans-PtCl2(NH3)}2-µ-(H2N(CH2)6NH2)]2+ (1,1/t,t) was the first of this series to show promising results, however, it was the trinuclear complex [{trans-PtCl2(NH3)}2-µ-trans-Pt(NH3)2(H2N(CH2)6NH2)2]4+ (1,0,1/t,t,t or BBR3464) that was chosen for clinical trials based on significantly increased cytotoxicity compared to 1,1/t,t and cisplatin. Molecular biology experiments have shown that 1,1/t,t exclusively forms IX

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31

Musetti, Caterina Livia. "Heterocyclic Cations as Potential Anticancer Agents: An Approach that Targets G-quadruplex with Different Binding Modes." Digital Archive @ GSU, 2010. http://digitalarchive.gsu.edu/chemistry_theses/26.

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G-quadruplex structures are found in important regions of the eukaryotic genome, such as telomeres and regulatory sequences of genes, and are likely to play important roles in regulation of biological events. The significant structural differences with duplex DNA make quadruplex DNA a very attractive target for anticancer drug design. The purpose of this study is to explore conformational space in a series of heterocyclic cations to discover novel structural motifs that can selectively bind and stabilize specific G-quadruplex arrangements. A variety of biophysical techniques such as thermal me

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32

Greco, Maria Laura. "Conformational switch of oncogene promotorial sequences towards non-canonical DNA secondary structures." Doctoral thesis, Università degli studi di Padova, 2015. http://hdl.handle.net/11577/3424026.

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The folding of DNA molecule into non-canonical secondary structures has been shown to be implicated in many important biological processes which regulate cell proliferation and proteins expression. In particular one of these peculiar secondary structures, called G-quadruplex (G4), has been shown to potentially impair cancer development. G4 occurs along DNA sequences rich of consecutive guanines which can fold through Hoostein pairs by forming stacked planes of guanines tetrads. This conformation prevalently forms along the termini of chromosomes (telomeres) but also along the promoter sites of

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33

Yang, Dazhou. "Synthesis and biophysical evaluation of thiazole orange derivatives as DNA binding ligands." Scholarly Commons, 2014. https://scholarlycommons.pacific.edu/uop_etds/141.

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Guanine-rich telomeric DNA at the end of chromosomes can form a unique DNA tertiary structure - G-quadruplex, which is known to inhibit the binding of telomerase to telomeric regions in cancer cells and thus regulate unrestricted cancer cell growth. Hence, G-quadruplex DNA has recently become a promising target in oncology. The formation of G-quadruplex structures is greatly facilitated by G-quadruplex binding ligands such as Thiazole orange (TO). Compared with other G-quadruplex binding ligands, TO has an intriguing tunable fluorescence property. Upon binding to DNA, the fluorescence of TO ca

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34

Klotz, Rémi. "Rôle de la protéine Damaged DNA Binding 2 dans la réponse des cellules tumorales mammaires aux agents thérapeutiques." Thesis, Université de Lorraine, 2014. http://www.theses.fr/2014LORR0134/document.

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Le laboratoire a récemment identifié la protéine Damaged-DNA-Binding 2 (DDB2), connue à l’origine pour son rôle dans la réparation de l’ADN comme une protéine impliquée dans la tumorigenèse mammaire. En effet, nous avons montré son rôle dans la croissance et la progression des tumeurs mammaires via la régulation transcriptionnelle de gènes cibles. Dans ce travail, nous avons montré que la surexpression de DDB2 augmente la sensibilité des cellules tumorales MDA-MB231 et SKBr3 traitées à la doxorubicine et au 5-fluorouracile (5-FU). Inversement, l’inhibition de l’expression de DDB2 dans les cell

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35

Cameron, Linda. "Elucidation of the sequence selective binding mode of the DNA minor groove binder adozelesin, by high-field ¹H NMR and restrained molecular dynamics." Thesis, University of Bath, 1999. https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.311174.

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36

Ali, Asfa. "New DNA-Targeting Small Molecules as Potential Anticancer Agents and for in vivo Specificity toward Enhanced Silk Production." Thesis, 2014. http://etd.iisc.ac.in/handle/2005/3514.

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The thesis entitled “New DNA-Targeting Small Molecules as Potential Anticancer Agents and for in vivo Specificity toward Enhanced Silk Production” encompasses design, computational calculations, and syntheses of diverse small molecular scaffolds to explicitly target duplex and higher order DNA morphologies (G-quadruplex DNA). Some of these molecules have a potential as anticancer agents. Besides, an attempt has been made elucidate the importance of novel oligopyrrole carboxamides in the enhancement of silk yield, hence proving to a boon in the field of sericulture. The work has been divided in

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37

Ali, Asfa. "New DNA-Targeting Small Molecules as Potential Anticancer Agents and for in vivo Specificity toward Enhanced Silk Production." Thesis, 2014. http://etd.iisc.ernet.in/2005/3514.

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The thesis entitled “New DNA-Targeting Small Molecules as Potential Anticancer Agents and for in vivo Specificity toward Enhanced Silk Production” encompasses design, computational calculations, and syntheses of diverse small molecular scaffolds to explicitly target duplex and higher order DNA morphologies (G-quadruplex DNA). Some of these molecules have a potential as anticancer agents. Besides, an attempt has been made elucidate the importance of novel oligopyrrole carboxamides in the enhancement of silk yield, hence proving to a boon in the field of sericulture. The work has been divided in

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38

Pages, Benjamin J. "Polyaromatic anticancer platinum complexes : synthesis and analysis of DNA binding." Thesis, 2018. http://hdl.handle.net/1959.7/uws:47363.

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Chemotherapy is a primary source of treatment for victims of cancer, a globally prominent disease that affects millions. The platinum(II) agents cisplatin, carboplatin and oxaliplatin are used in approximately half of all chemotherapy treatment schemes. These drugs kill cancerous cells by binding covalently to DNA and preventing replication, which leads to apoptosis. Despite the success of these drugs they have many debilitating side effects such as nephrotoxicity, myelotoxicity, nausea and vomiting. Furthermore, many cancers are resistant to treatment from these drugs, often through DNA repai

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Chorna, Ielyzaveta. "Evaluation of the binding of vanadium-based anticancer drugs to human serum proteins." Master's thesis, 2015. http://hdl.handle.net/10400.1/7947.

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Dissertação de mestrado, Qualidade em Análises, Faculdade de Ciências e Tecnologia, Universidade do Algarve, 2015<br>Oxidovanadium(IV) complexes, namely those containing organic polydentade ligands, often designated by VO8carrier)n compounds, have attracted a great interest due to their prospective therapeutic effects, particularly in the treatment of diabetes, cancer and diseases caused by parasites.

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Brabec, V., S. E. Howson, R. A. Kaner, et al. "Metallohelices with activity against cisplatin-resistant cancer cells; does the mechanism involve DNA binding?" 2013. http://hdl.handle.net/10454/9486.

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Yes<br>Enantiomers of a relatively rigid DNA-binding metallo-helix are shown to have comparable activity to that of cisplatin against the cell lines MCF7 (human breast adenocarcinoma) and A2780 (human ovarian carcinoma) but are ca five times more active against the cisplatin-resistant A2780cis. The cell-line HCT116 p53+/+ (human colon carcinoma) is highly sensitive giving IC50 values in the nM range, far lower than the cisplatin control. The hypothesis that the biological target of such metallohelices is DNA is probed by various techniques. Tertiary structure changes in ct-DNA (formation

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41

Patterson, Laurence H., Klaus Pors, Steven D. Shnyder, et al. "Synthesis of DNA-Directed Pyrrolidinyl and Piperidinyl Confined Alkylating Chloroalkylaminoanthraquinones: Potential for Development of Tumor-Selective N-Oxides." 2006. http://hdl.handle.net/10454/3060.

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No<br>A novel series of 1,4-disubstituted chloroethylaminoanthraquinones, containing alkylating chloroethylamino functionalities as part of a rigid piperidinyl or pyrrolidinyl ring-system, have been prepared. The target compounds were prepared by ipso-displacement of halides of various anthraquinone chromophores by either hydroxylated or chlorinated piperidinyl- or pyrrolidinyl-alkylamino side chains. The chloroethylaminoanthraquinones were shown to alkylate guanine residues of linearized pBR322 (1¿20 ¿M), and two symmetrically 1,4-disubstituted anthraquinones (compounds 14 and 15) were shown

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42

Hou, Ming-Hon, and 侯明宏. "The mechanistic study of GpC specific DNA-binding drugs bound to DNA duplexes and their potential application in disease therapy." Thesis, 2003. http://ndltd.ncl.edu.tw/handle/40217604833076064200.

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博士<br>國立臺灣大學<br>生化科學研究所<br>91<br>Many drugs and antibiotics are known to interact with DNA in order to exert their biological activities. The three-dimensional structures of several DNA-antitumor drug complexes have been determined by high resolution X-ray diffraction and other biophysical methods. These results have provided significant insights into DNA conformations and drug-DNA interactions to design useful novel drugs. There are several different interaction modes between drugs and DNA, namely, intercalation (such as daunorubicin and doxorubicin), groove-binding (such as distamycin A),

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Hussain, Akhtar. "Studies On Lanthanide Complexes Showing Photo-activated DNA Cleavage And Anticancer Activity." Thesis, 2011. https://etd.iisc.ac.in/handle/2005/2428.

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This thesis work deals with different aspects of the chemistry of La(III) and Gd(III) complexes, their interaction with DNA and proteins, photo-induced cleavage of double-stranded DNA, photocytotoxic effect on cancer cells, cell death mechanism and cellular localization behaviour. Chapter I gives an introduction to the metal-based anticancer agents with special emphasis on clinically used drugs and the growing field of lanthanide therapeutics. An overview of the current strategies of cancer treatment, especially photodynamic therapy (PDT), is presented. Mode of small molecule-DNA interacti

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Hussain, Akhtar. "Studies On Lanthanide Complexes Showing Photo-activated DNA Cleavage And Anticancer Activity." Thesis, 2011. http://etd.iisc.ernet.in/handle/2005/2428.

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This thesis work deals with different aspects of the chemistry of La(III) and Gd(III) complexes, their interaction with DNA and proteins, photo-induced cleavage of double-stranded DNA, photocytotoxic effect on cancer cells, cell death mechanism and cellular localization behaviour. Chapter I gives an introduction to the metal-based anticancer agents with special emphasis on clinically used drugs and the growing field of lanthanide therapeutics. An overview of the current strategies of cancer treatment, especially photodynamic therapy (PDT), is presented. Mode of small molecule-DNA interactio

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Wang, I.-Chun, and 王義政. "The influence of methylenetetrahydrofolate reductase polymorphism, nutritional status and anticancer drugs on one-carbon metabolic fluxes pathway and DNA methylation." Thesis, 2005. http://ndltd.ncl.edu.tw/handle/18067749358036228118.

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碩士<br>國立中興大學<br>食品科學系<br>93<br>Genetic predisposition plays a significant role in tumorigenesis and cancer prevention. A common polymorphism 677C->T in methylenetetrahydrofolate reductase (MTHFR) is associated with altered risk of certain types of cancer, but the mechanism remains to be determined. MTHFR catalyzes the reduction of 5, 10-methylene- tetrahydrofolate to 5-methyltetrahydrofolate, the methyl donor for the synthesis of methionine from homocysteine. The homozygous C677T mutation in the MTHFR gene results in reduction in enzyme activity and changes in cellular distribution of folates.

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Rettig, Michael [Verfasser]. "Thermodynamic and NMR structural studies on the DNA binding of bifunctional drugs with alkylating activity / vorgelegt von Michael Rettig." 2010. http://d-nb.info/1002425433/34.

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Wells, G., Marie Suggitt, M. Coffils, et al. "Fluorescent 7-Diethylaminocoumarin Pyrrolobenzodiazepine conjugates: Synthesis, DNA-Interaction, Cytotoxicity and Differential Cellular Localization." 2008. http://hdl.handle.net/10454/4569.

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no<br>The pyrrolo[2,1-c][1,4]benzodiazepines (PBDs) are a class of DNA minor groove binding agents that react covalently with guanine bases, preferably at Pu-G-Pu sites. A series of three fluorescent PBD¿coumarin conjugates with different linker architectures has been synthesized to probe correlations between DNA binding affinity, cellular localization and cytotoxicity. The results show that the linker structure plays a critical role for all three parameters. Graphical abstract A series of three fluorescent PBD¿coumarin conjugates with different linker architectures has been synthesized to p

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Krzak, Agata. "Modyfikowane cyklodekstryny jako nośniki leków i ich oddziaływania z DNA." Doctoral thesis, 2021. https://depotuw.ceon.pl/handle/item/4001.

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Tematyka pracy doktorskiej dotyczy modyfikowanych cyklodekstryn jako nośników leków. Na początku pracy podano spis stosowanych skrótów oraz wyjaśniono cele pracy doktorskiej. Część literaturowa składa się z czterech rozdziałów. Rozdział pierwszy zawiera opis budowy, właściwości cyklodekstryn oraz ich zastosowań w przemyśle farmaceutycznym jako nośników leków. Następny rozdział poświęcono scharakteryzowaniu kwasu deoksyrybonukleinowego, jego budowie i strukturze, oraz możliwym sposobom oddziaływania związków chemicznych z DNA. W rozdziale trzecim omówiono budowę oraz mechanizm działania temozol

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Huang, Wei. "Small molecule compounds targeting DNA binding domain of STAT3 for inhibition of tumor growth and metastasis." Thesis, 2014. http://hdl.handle.net/1805/5221.

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Indiana University-Purdue University Indianapolis (IUPUI)<br>Signal transducer and activator of transcription 3 (STAT3) is constitutively activated in malignant tumors, and its activation is associated with high histological grade and advanced cancer stage. STAT3 has been shown to play important roles in multiple aspects of cancer aggressiveness including proliferation, survival, self-renewal, migration, invasion, angiogenesis and immune response by regulating the expression of diverse downstream target genes. Thus, inhibiting STAT3 promises to be an attractive strategy for treatment of advanc

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Babu, Balaji. "Studies on Photocytotoxic Ferrocenyl Conjugates." Thesis, 2014. http://etd.iisc.ac.in/handle/2005/3028.

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The present thesis deals with different aspects of the chemistry and photo-biology of various ferrocene-conjugates, their interaction with double helical DNA, DNA photocleavage and photo-enhanced cytotoxicity in visible light, localization and cellular uptake to study the mechanism of cell death. Phenyl analogues of the active complexes have been synthesized and used for comparison in biological assays. Chapter I presents an overview of cancer and its types, various treatments for cancer. A general overview on the Photodynamic Therapy, a new modality of light activated cancer treatment and i

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