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Dissertations / Theses on the topic 'Inhibitors compounds'

Author: Grafiati

Published: 4 June 2021

Last updated: 2 February 2022

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1

Tan, Swee Hain. "Organic corrosion inhibitors." Murdoch University, 1991. http://wwwlib.murdoch.edu.au/adt/browse/view/adt-MU20060818.150145.

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The overall aims of this thesis were to conduct a broad survey of possible organic corrosion inhibitors in near-neutral chloride solutions and to elucidate the mechanisms of such action. Altogether, 130 organic compounds were studied as possible corrosion inhibitors for pure iron, mild steel, copper and aluminium in aerated near-neutral (pH = 8.4) solutions containing 500 ppm NaCl and 100 ppm NaHCO,, conditions often encountered in water-based automotive engine coolants. Inhibitor behaviour was investigated using steady-state electrochemical techniques including polarisation curves, Stern-Gear

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2

Geraets, Liesbeth. "Dietary PARP-1 inhibitors as anti-inflammatory compounds." Maastricht : Maastricht : Universitaire Pers ; University Library, Universiteit Maastricht [host], 2008. http://arno.unimaas.nl/show.cgi?fid=14252.

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3

McNab, Donald. "Boron-containing compounds as inhibitors of HIV proteinase." Thesis, University of St Andrews, 1997. http://hdl.handle.net/10023/14305.

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HIV Proteinase (HIV PR) has proved to be an excellent target for the development of anti-AIDS drugs. Four inhibitors of this enzyme are now approved for clinical use but they, like others, suffer from shortcomings associated with their size and the fact they are peptides. In this thesis the development of small non-peptidic cyclic compounds is described. They were designed to inhibit HIV PR principally by targeting its unique structural features rather than by mimicking its natural substrates. The designed compounds all contained the borinic acid functional group which it was anticipated would

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4

Corredor, Sánchez Miriam. "Chemical Modulation of Identified Hit Compounds as Apoptosis Inhibitors." Doctoral thesis, Universitat Ramon Llull, 2013. http://hdl.handle.net/10803/117361.

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L’apoptosi és un procés biològic rellevant en moltes malalties. Un punt de regulació d’aquest procés és la formació d’un complex multiproteic anomenat apoptosoma; per tant, aquest complex té un gran interès per al desenvolupament de moduladors apoptòtics. El nostre grup ha descrit prèviament una piperazina-2,5-diona substituïda en posició 3 com a potent modulador apoptòtic. Estudis estructurals d’aquest compost han permès veure la presència dels isòmers cis / trans de l’enllaç de l’amida terciària exocíclica en un procés d’intercanvi lent, fet que pot ser important per a la interacció amb la d

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5

Ryle, Peter Robert. "Ethanol-induced fatty liver : protective action of (+)-catechin compounds." Thesis, University of Surrey, 1986. http://epubs.surrey.ac.uk/847975/.

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The aim of the work presented in this thesis was to assess the protective properties of the bioflavanoid drug, (+)-catechin, and its palmityl ester, 3-palmitoyl-(+)-catechin, against ethanol hepato-toxicity (ie: fatty liver) in the rat. In initial experiments, both (+)-catechin compounds were found to protect against the hepatic lipid accumulation (mainly triglyceride) after acute ethanol dosing, and after long-term feeding of ethanol in a liquid diet. In the latter situation, 3-palmitoyl-(+)-catechin was significantly more effective than (+)-catechin itself at preventing fatty liver, probably

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6

Abner, Erik 1986. "Identification of HIV-1 reactivating quinoline compounds as bromodomain inhibitors." Doctoral thesis, Universitat Pompeu Fabra, 2016. http://hdl.handle.net/10803/565528.

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Tras la infección por VIH-1, el establecimiento de un depósito de células T en reposo infectadas latentemente con VIH impide la erradicación del virus en pacientes. Para lograr la erradicación, la terapia retroviral existente debe combinarse con medicamentos que reactiven los virus latentes. Previamente, nuestro grupo describió un nuevo compuesto químico, MMQO (8-metoxi-6-metilquinolin-4-ol) que es capaz de reactivar la transcripción viral a través de un mecanismo desconocido. El objetivo de este proyecto fue identificar los proteínas que interaccionan con MMQO e investigar su papel en la reac

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7

Cunningham, Bernadette D. M. "Flavones and related compounds as inhibitors of protein tyrosine kinases." Thesis, Aston University, 1987. http://publications.aston.ac.uk/12513/.

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Aberrant tyrosine protein kinase activity has been implicated in the formation and maintenance of malignancy and so presents a potential target for cancer chemotherapy. Quercetin, a naturally occuring flavonoid, inhibits the tyrosine protein kinase encoded by the Rous sarcoma virus but also exhibits many other effects. Analogues of this compound were synthesised by the acylation of suitable 2-hydroxyacetophenones with appropriately substituted aromatic (or alicyclic) acid chlorides, followed by base catalysed rearrangement to the 1-(2-hydroxyphenyl)-3-phenylpropan-1,3-diones. Acid catalysed ri

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8

García, Reyes Balbina [Verfasser]. "Validation of new Casein Kinase 1 (CK1) small molecule inhibitor compounds and characterization of Inhibitors of Wnt Production (IWPs) as inhibitors of CK1δ / Balbina García Reyes". Ulm : Universität Ulm, 2018. http://d-nb.info/1151938424/34.

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9

Byrom, Daniel. "Synthesis of TGF-Beta inhibitors and compounds for spatiotemporal drug release." Doctoral thesis, Universitat de Barcelona, 2018. http://hdl.handle.net/10803/665149.

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During this doctoral thesis, we have synthesised hundreds of grams of the TGF-β inhibitor LY2157299 (Galunisertib). This product was used by the group of Eduard Batlle in their investigations into the roles that TGF-β plays in colorectal cancer. During the initial synthesis and subsequent scale up, we overcame hurdles including optimisation of the penultimate step of the reaction - giving reproducible results - as well as optimising conditions of the final solid form to provide a product which is suitable for formulation for the in vivo experiments. After discovering some of the drawback of LY

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10

Omune, Duncan Otieno. "Synthetic analogs of equisetin as potential HIV-1 integrase inhibitors." Diss., Online access via UMI:, 2004. http://wwwlib.umi.com/dissertations/fullcit/3150487.

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11

Vasquez, Valdivieso Montserrat Guadalupe. "Identification of selective inhibitors of phosphofructokinase and fructose bisphosphatase as lead compounds against trypanosomatids." Thesis, University of Edinburgh, 2014. http://hdl.handle.net/1842/17980.

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Trypanosomatid parasites cause a wide range of so-called neglected diseases which affect over 27 million people every year. Current treatments are toxic and prone to resistance; therefore, it is imperative to identify novel protein targets and to develop more efficient treatments. Phosphofructokinase (PFK) is the third enzyme in glycolysis, and its reciprocal enzyme in gluconeogenesis is fructose-1,6-bisphosphatase (FBPase); in trypanosomatid parasites (Trypanosoma brucei [Tb], Trypanosoma cruzi [Tc] and Leishmania [Lm] species), both enzymes are recognised drug targets. This thesis describes

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12

Sebesho, Biopelo Felicity. "Investigation of the efficacy of identified acetolactate synthase inhibitors, peptidyl cysteine protease inhibitors, thiolactomycins, and thiosemicarbazone compounds against Mycobacterium tuberculosis." Master's thesis, University of Cape Town, 2006. http://hdl.handle.net/11427/3116.

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Includes bibliographical references (leaves 131-141).<br>Tuberculosis remains an important public health problem worldwide. There has been increase in the development of drug resistance towards INH and RIF, two of the frontline antimycobacterial drugs currently used in therapeutic regimes. As an attempt to address drug resistance, the World Health Organization has implemented the DOTS strategy in 182 countries. Moreover, new chemical libraries of potential antituberculosis drugs have been designed and synthesised. We therefore assessed 121 derivatives from the acetolactate synthase inhibitors,

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13

Sekgota, Khethobole Cassius. "Design, development and evaluation of novel lead compounds as HIV-1 enzyme inhibitors." Thesis, Rhodes University, 2015. http://hdl.handle.net/10962/d1017926.

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This project has been concerned with the application of the Baylis-Hillman methodology to the synthesis of medicinally important diketo acid analogues (cinnamate ester-AZT conjugates and 3-hydroxy ester-AZT conjugates) as dual-action HIV-1 IN/RT inhibitors; and on exploratory studies in the preparation of 3-(amidomethyl)-(1H)-2-quinolones as PR inhibitors; and (1H)-2- quinolone-AZT conjugates as dual action IN/RT inhibitors. A series of Baylis-Hillman adducts has been prepared, typically in moderate to excellent yield, by reacting 2-nitrobenzaldehyde with methyl acrylate, ethyl acrylate and me

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14

Muto, Yukiyo. "The synthesis and mode of action of NPPB and related compounds." Thesis, University of Canterbury. Biological Sciences, 2006. http://hdl.handle.net/10092/1522.

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5-nitro-2-(3-phenylpropylamino)-benzoic acid (NPPB) was normally recognised as a Cl- channel inhibitor, but its specificity is in question, since an inhibitory effect against K⁺ channels has been reported. To identify the significance of the molecules structural components, NPPB and related compounds, such as 2-(3-phenylpropylamino) benzoic acid (PPAB), 5- nitro-2-heptylamino benzoic acid (HANB) and 2-nitro-5-heptylamino benzoic acid (HANB-2) were synthesised by reductive amination using various aldehydes and amines. Using internodal cells of the giant green Characean algae, Nitella hookeri, t

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15

Tamakawa, Raina Ayako. "Combination chemotherapy with telomerase inhibitors and genotoxic compounds against breast and colorectal cancers." Thesis, University of British Columbia, 2010. http://hdl.handle.net/2429/29124.

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Telomerase is the specialized reverse transcriptase responsible for the de novo synthesis of telomeric repeats at chromosome ends. Telomerase plays important roles in tumor development and is responsible for the indefinite growth phenotype in cancer. Telomerase over-expression is found in more than 85% of human tumors surveyed. In contrast, normal somatic cells have low or undetectable telomerase expression, making the enzyme an appealing target for the development of anticancer therapy. However, there is a significant time lag between the start of telomerase inhibition therapy and growth i

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16

Majgier-Baranowska, Helena. "Studies in the synthesis of mechanism-based steroid enzyme inhibitors and related compounds." Thesis, National Library of Canada = Bibliothèque nationale du Canada, 1998. http://www.collectionscanada.ca/obj/s4/f2/dsk3/ftp04/nq23633.pdf.

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17

Nokalipa, Iviwe Cwaita. "Synthesis and bioassay of rationally designed DXR inhibitors as potential antimalarial lead compounds." Thesis, Rhodes University, 2017. http://hdl.handle.net/10962/4888.

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Globally, the eradication of malaria has been challenging due to the problem of resistance that past and currently available drugs exhibit. This is exacerbated by the inherent need for anti-malarial drugs to be affordable to the poverty-stricken majority that is primarily affected by this burden. This research has focused on the development of potential inhibitors of 1-deoxy-D- xylulose-5 phosphate reductoisomerase (DXR), an essential enzyme in the mevalonate- independent pathway for the biosynthesis of isoprenoids in Plasmodium falciparum. DXR mediates the isomerisation and reduction of 1-deo

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18

Chojnacki, Jeremy E. "NOVEL COMPOUNDS AS POTENTIAL ALZHEIMER'S DISEASE THERAPEUTICS AND INHIBITORS OF THE NLRP3 INFLAMMASOME." VCU Scholars Compass, 2014. http://scholarscompass.vcu.edu/etd/3616.

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Alzheimer’s disease is a devastating neurodegenerative disorder and the leading cause of dementia. The disease manifests via several pathologies including neuroinflammation, oxidative stress, metal ion dyshomeostasis, and cell death. To address the multifaceted nature of this disorder, the design of several diverse compounds, targeting many pathological effects, was generated. First, a series of compounds based on curcumin and diosgenin were synthesized following the bivalent design strategy. Two compounds were discovered to have neuroprotective ability, anti-oxidative function, and anti-Aß ol

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19

Gheura, Iuliana L. "Design, synthesis and evaluation of AZA-peptide epoxides as inhibitors of cysteine proteases." Diss., Georgia Institute of Technology, 2002. http://hdl.handle.net/1853/30571.

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20

Zou, Taotao, and 邹滔滔. "Anti-cancer N-heterocyclic carbene complexes of gold(III), gold(I) and platinum(II) : thiol "switch-on" fluorescent probes, thioredoxin reductase inhibitors and endoplasmic reticulum targeting agents." Thesis, The University of Hong Kong (Pokfulam, Hong Kong), 2015. http://hdl.handle.net/10722/208614.

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21

Li, Ka-lei Carrie. "In vitro and in vivo studies of cytotoxic and anti-angiogenic cyclometalated gold(III) and gold(III) porphyrin complexes." Click to view the E-thesis via HKUTO, 2008. http://sunzi.lib.hku.hk/hkuto/record/B39634577.

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22

Li, Ka-lei Carrie, and 李嘉莉. "In vitro and in vivo studies of cytotoxic and anti-angiogenic cyclometalated gold(III) and gold(III) porphyrin complexes." Thesis, The University of Hong Kong (Pokfulam, Hong Kong), 2008. http://hub.hku.hk/bib/B39634577.

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23

Concia, Alda Lisa. "Chemoenzymatic synthesis of sugar-related polyhydroxylated compounds, iminocyclitols and their derivatives as glycosidase inhibitors." Doctoral thesis, Universitat de Barcelona, 2013. http://hdl.handle.net/10803/113239.

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Section 1 (Introduction) is a comprehensive review of the subjects discussed in this thesis: biocatalysis, aldolases and iminocyclitols. It contains a description of the application of dihydroxyacetone phosphate (DHAP) and dihydroxyacetone (DHA) utilizing aldolases to the chemoenzymatic synthesis of bioactive compounds and an introduction to the structure, biological activities and synthesis of iminocyclitols. Recent bibliographic references are included at the end of the section. Section 2 (Objectives) outlines the aims of this thesis. Section 3 (Results and discussion) describes the stud

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24

Latorre, Martínez Antonio. "Studies of sulfurated compounds and epoxidation of MDH adducts. New inhibitors of cysteine proteases." Doctoral thesis, Universitat Jaume I, 2015. http://hdl.handle.net/10803/669020.

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A. L. Martínez presents a PhD thesis on syntheses design and testing of new protease inhibitors targeting proteasome and cysteine proteases, e.g. cathepsins. With the various chapters his thesis covers fields from organic chemistry and medicinal chemistry, it includes detailed mechanistic studies on reaction mech- anisms and stereochemical output of the reactions. In chapter 1 A. L. Martínez presents his work on syntheses of unsaturated compounds from sulfinyl esters by elimination reaction. His detailed and very systematic studies resulted in a proposal for a complete reaction pathway whi

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25

Ovat, Asli. "Design, synthesis and evaluation of cysteine protease inhibitors." Diss., Georgia Institute of Technology, 2009. http://hdl.handle.net/1853/33822.

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Cysteine proteases are important drug targets due to their involvement in many biological processes such as protein turnover, digestion, blood coagulation, apoptosis, cell differentiation, cell signaling, and the immune response. In this thesis, we have reported the design, synthesis and evaluation of clan CA and clan CD cysteine protease inhibitors. Aza-peptidyl Michael acceptor and epoxide inhibitors for asparaginyl endopeptidases (legumains) from the bloodfluke, Schistosoma mansoni (SmAE) and the hard tick, Ixodes ricinus (IrAE) were designed and synthesized. SARs were similar, but with s

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26

Hodson, Luke. "The synthesis of novel kinase inhibitors using click chemistry." Thesis, Stellenbosch : Stellenbosch University, 2014. http://hdl.handle.net/10019.1/86704.

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Thesis (MSc)--Stellenbosch University, 2014.<br>ENGLISH ABSTRACT: Cancer is the leading cause of death on the planet, killing an estimated 8.2 million people in the year of 2012.The disease is associated with two families of genes, namely oncogenes and tumour suppressor genes. The hallmarks of cancer pathogenesis include gene amplification, point mutations or chromosomal rearrangements within these genes. Kinases are responsible for the reversible phosphorylation of proteins, which plays a significant and extensive role in cellular signal transduction. Aberrant kinase activity provokes overexp

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27

Ruell, Jeffrey Alan. "Synthetic and theoretical studies of polyanionic inhibitors of HIV-1 infection of CD4-expressing cells." Diss., Georgia Institute of Technology, 1995. http://hdl.handle.net/1853/30987.

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28

Rose, Nathan Rolf. "Synthesis of novel coumarin derivatives as potential inhibitors of HIV-1 protease." Thesis, Rhodes University, 2007. http://hdl.handle.net/10962/d1007220.

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This research has focused on the development of novel coumann derivatives containing peptide-like side chains as potential HIV-1 protease inhibitors. The reaction of various salicylaldehyde derivatives with tert-butyl acrylate In the presence of 1,4- diazabicyclo[2.2.2]octane (DABCO) has afforded a series of Baylis-Hillman adducts in moderate yield. Cyclisation of the adducts in the presence of HCI afforded the corresponding 3-(chloromethyl)coumarin derivatives, which have been reacted with various amine hydrochlorides in the presence of Proton Sponge® to afford a series of novel 3- (aminometh

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29

Manzo, Stefano Giustino <1986&gt. "Natural compounds Camptothecin and Triptolide: highly specific enzyme inhibitors and tools to dissect transcriptional functions." Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2015. http://amsdottorato.unibo.it/6961/.

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With this work I elucidated new and unexpected mechanisms of two strong and highly specific transcription inhibitors: Triptolide and Campthotecin. Triptolide (TPL) is a diterpene epoxide derived from the Chinese plant Trypterigium Wilfoordii Hook F. TPL inhibits the ATPase activity of XPB, a subunit of the general transcription factor TFIIH. In this thesis I found that degradation of Rbp1 (the largest subunit of RNA Polymerase II) caused by TPL treatments, is preceded by an hyperphosphorylation event at serine 5 of the carboxy-terminal domain (CTD) of Rbp1. This event is concomitant with a

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30

La, Rosa Salvatore. "Design and synthesis of GTPCH-I inhibitors and related compounds via solution and solid phase." Thesis, University of Strathclyde, 2002. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.248732.

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31

O'Donnell, Valerie Bridget. "Iodonium compounds as inhibitors of neutrophil NADPH oxidase and other flavin-containing electron transfer systems." Thesis, University of Bristol, 1992. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.333904.

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32

Wilson, Tyler Aron. "Design and Synthesis of Novel Bioactive Compounds for the Development of HIV-1 Allosteric Integrase Inhibitors, 20S Proteasome Inhibitors, and Anticancer Natural Product Derivatives." The Ohio State University, 2019. http://rave.ohiolink.edu/etdc/view?acc_num=osu1565967461685907.

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33

Rashamuse, Thompho Jason. "Studies towards the synthesis of novel, coumarin-based HIV-1 protease inhibitors." Thesis, Rhodes University, 2008. http://eprints.ru.ac.za/1332/.

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34

Tukulula, Matshawandile. "The design and synthesis of novel HIV-1 protease inhibitors." Thesis, Rhodes University, 2009. http://eprints.ru.ac.za/1563/.

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35

Cousin, D. "New synthetic routes to the angiogenesis inhibitors combretastatin D2 and the compounds of the ICM0301 family." Thesis, Queen's University Belfast, 2008. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.479251.

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36

Row, Eleanor Catherine. "Design, synthesis and evaluation of coumarin and furanocoumarin compounds as inhibitors of CYP3A4 and P-glycoprotein." Thesis, University of Sheffield, 2003. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.401162.

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37

Vaitiekutė, Justina. "Membranas laidinančių medžiagų ir daugiavaisčio atsparumo siurblių slopiklių poveikis bakterijų sąveikai su TPP+ jonais." Master's thesis, Lithuanian Academic Libraries Network (LABT), 2014. http://vddb.library.lt/obj/LT-eLABa-0001:E.02~2009~D_20140626_190654-65889.

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Šio darbo tikslas buvo ištirti antimikrobinių medžiagų ir daugiavaisčio atsparumo siurblių slopiklių poveikį bakterijų sąveikai su TPP+ jonais. Šiam tikslui pasiekti reikėjo ištirti antimikrobinių peptidų įtaką bakterinių apvalkalėlių laidumui, įvertinti M. smegmatis bakterijų apvalkalėlio sąveiką su TPP+ jonais ir jų pasiskirstymą veikiant šias polikatijoniniais junginiais bei ištirti daugiavaisčio atsparumo siurblių slopiklių įtaką TPP+ jonų pasiskirstymui abipus M. smegmatis bakterijų apvalkalėlio. Šio darbo metu buvo parodyta, kad peptidų pVEC ir cys-pVEC sąveika su gramneigiamųjų E. coli

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38

Abuelyaman, Ahmed Salih. "Synthesis and evaluation of fluorescent and biotinylated derivatives of diphenyl peptidylphosphonate esters and biotinylated isocoumarins as inhibitors of serine proteases." Diss., Georgia Institute of Technology, 1994. http://hdl.handle.net/1853/27556.

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Ersmark, Karolina. "Design and Synthesis of Malarial Aspartic Protease Inhibitors." Doctoral thesis, Uppsala : Acta Universitatis Upsaliensis : Univ.-bibl. [distributör], 2005. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-4833.

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Örtqvist, Pernilla. "On the Design and Synthesis of Hepatitis C Virus NS3 Protease Inhibitors : From Tripeptides to Achiral Compounds." Doctoral thesis, Uppsala universitet, Avdelningen för organisk farmaceutisk kemi, 2010. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-110738.

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Infection by the hepatitis C virus (HCV) leads to inflammation of the liver, i.e. hepatitis. The acute infection often progresses to a chronic phase during which the liver function is gradually impaired. Approximately 20% of these chronic cases develop liver cirrhosis, with an ensuing increased risk of liver cancer. Global estimates of the total number of chronic cases range from 123–170 million. Yet, neither specific anti-HCV drugs nor vaccines are available. When drugs become available for daily clinical use, rapid development of drug-resistant strains is expected, making resistance an impor

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Nikjoo, Dariush. "Design and Synthesis of a Small Set of Thiourea-based Compounds as Inhibitors of AChE1 from Mosquitoes." Thesis, Umeå universitet, Kemiska institutionen, 2014. http://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-92551.

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Johnson, Bernadette. "Fluorinated #alpha#-amino acid analogues of L-methionine and related compounds for use as potential enzyme inhibitors." Thesis, University of Glasgow, 1998. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.264261.

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Örtqvist, Pernilla. "On the design and synthesis of hepatitis C virus NS3 protease inhibitors : from tripeptides to achiral compounds /." Uppsala : Acta Universitatis Upsaliensis, 2010. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-110738.

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Lee, Yi-Chen. "Studies towards the development of novel HIV-1 integrase inhibitors." Thesis, Rhodes University, 2010. http://hdl.handle.net/10962/d1005022.

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The project has focused on the preparation of several series of compounds designed as potential HIV-1 integrase inhibitors. Various 2-nitrobenzaldehydes have been reacted with two activated alkenes, methyl vinyl ketone (MVK) and methyl acrylate, under Baylis-Hillman conditions to afford α-methylene-β-hydroxylalkyl derivatives in moderate to excellent yields. The reactions were conducted using the tertiary amine catalysts, 1,4-diazabicyclo[2.2.2]octane(DABCO) or 3-hydroxyquinuclidine (3-HQ) with chloroform as solvent, and yields were optimised by varying the catalyst, reagent concentrations and

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Prior, Allan Mark. "Synthesis and anti-viral activity of novel tripeptidyl compounds, modification of graphene oxides, and synthesis of peptidyl substrates for use in an electrochemical biosensor device." Diss., Kansas State University, 2013. http://hdl.handle.net/2097/27654.

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Doctor of Philosophy<br>Department of Chemistry<br>Duy H. Hua<br>Three research projects are described in this dissertation and they consist of the discovery of norovirus protease inhibitors, modification of graphene oxides (GO) for the detection of norovirus, and design and fabrication of nanoelectronic device based on nanocarbon fibers for the detection of breast cancer proteases, legumain and cathepsin B. A novel class of tripeptidyl anti-noroviral compounds which strongly inhibit NV3CL[superscript]pro in enzyme and cell based assays was discovered. An example of one of the most active com

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Scrivens, Paul James. "Regulation and chemotherapeutic targeting of human Cdc25A phosphatase." Thesis, McGill University, 2007. http://digitool.Library.McGill.CA:80/R/?func=dbin-jump-full&object_id=103293.

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The Cdc25 phosphatases are highly conserved from yeast through humans and play pivotal roles in regulating the activities of cyclin-dependent kinases (Cdks). Cdc25A is one of three human Cdc25 family members, and has previously been shown to be overexpressed in numerous cancers and to transform rodent fibroblasts. Cdc25A therefore represents a rational target for chemotherapeutic development. Further, a thorough understanding of its biology and regulation in normal and transformed cells may facilitate the development of strategies to specifically interfere with the proliferation of cancerous c

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Mutorwa, Marius Kudumo. "Synthesis of novel inhibitors of 1-Deoxy-D-xylulose-5-phosphate reductoisomerase as potential anti-malarial lead compounds." Thesis, Rhodes University, 2011. http://hdl.handle.net/10962/d1005037.

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This research has focused on the development of novel substrate mimics as potential DXR inhibitors of 1-deoxy-D-xylulose-5-phosphate reductoisomerase (DXR), an essential enzyme in the mevalonate-independent pathway for the biosynthesis of isoprenoids in Plasmodium falciparum. DXR mediates the isomerisation and reduction of 1-deoxy-D-xylulose-5-phosphate (DOXP) into 2C-methyl-D-erithrytol 4-phosphate (MEP) and has been validated as an attractive target for the development of novel anti-malarial chemotherapeutic agents. Reaction of various amines with specially prepared 4-phosphonated crotonic a

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Richmond, Oliver H. III. "Extraction, Purification and Evaluation of PRMT5-Inhibitory Phytochemical Compounds for the Treatment of Prostate Adenocarcinoma." DigitalCommons@Robert W. Woodruff Library, Atlanta University Center, 2019. http://digitalcommons.auctr.edu/cauetds/185.

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The development and advancement of prostate cancer is supported by a plethora of genetic and proteomic abnormalities, including events of post-translational modifications. The protein arginine methyltransferase 5 (PRMT5) enzyme regulates epigenetic events of histone modifications and protein post-translational modifications within protein signaling pathways. PRMT5 functions by catalyzing the symmetric dimethylation of terminal arginine residues on target protein substrates. Under abnormal conditions of overexpression and upregulation, PRMT5 methyltransferase activity constitutively drives the

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49

Ella-Menye, Jean-Rene. "Synthesis of Novel Chiral Heterocyclic Compounds for Antibacterial Agents and Peptidomimetics." ScholarWorks@UNO, 2007. http://scholarworks.uno.edu/td/611.

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Small chiral molecules are very important building blocks in the synthesis of biologically active compounds. These building blocks include nitrogen and oxygen-containing heterocycles such as 2-oxazolidinones, 1,3-oxazinan-2-ones, 2-oxazolines, oxazines, morpholine and morpholinones. Because of their interesting properties, chiral heterocycles have stirred great interest in the synthetic chemist community to develop useful and efficient strategies to these molecules. In this dissertation, the design and syntheses of various heterocyclic building blocks are presented, as well as the testing of t

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Sayer, J. R. "The synthesis of imidazo[1,2-a]pyrazines as inhibitors of the VirB11 ATPase and their incorporation into bivalent compounds." Thesis, University College London (University of London), 2013. http://discovery.ucl.ac.uk/1398301/.

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Helicobacter pylori are gram negative bacteria that colonise in the human stomach causing illnesses such as peptide ulcers and various cancers. Through targeting a component of their secretion apparatus, it is envisaged that translocation of toxic molecules will be inhibited and therefore virulence would be reduced. Virtual high throughput screening of the Helicobacter pylori VirB11 ATPase, HP0525, identified imidazo[1,2-a]pyrazine compounds as potential ATP mimics and ATPase inhibitors. Synthesis of these target compounds was carried out, with two routes established to deliver 2- and 3- aryl

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