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Dissertations / Theses on the topic 'Derivatives of pyrimidine'

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Published: 5 June 2025

Last updated: 1 August 2025

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1

Hill, Matthew D. (Matthew Dennis). "Direct synthesis of pyridine and pyrimidine derivatives." Thesis, Massachusetts Institute of Technology, 2008. http://hdl.handle.net/1721.1/43776.

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Thesis (Ph. D.)--Massachusetts Institute of Technology, Dept. of Chemistry, 2008.<br>Vita.<br>Includes bibliographical references.<br>I. Synthesis of Substituted Pyridine Derivatives via the Ruthenium-Catalyzed Cycloisomerization of 3-Azadienynes. The two-step conversion of various N-vinyl and N-aryl amides to the corresponding substituted pyridines and quinolines, respectively, is described. The process involves the direct conversion of amides, including sensitive N-vinyl amides, to the corresponding trimethylsilyl alkynyl imines followed by a ruthenium-catalyzed protodesilylation and cyclois

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2

Chan, Heng Ming. "Synthesis of pyrimidine C-nucleoside analogues and triphosphate derivatives." Thesis, Boston College, 2008. http://hdl.handle.net/2345/36.

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Five pyrimidine C-nucleosides were prepared via Heck-type coupling reactions. These derivatives are designed to mimic dC and dU (or T). The minor groove O2 carbonyl in each derivative is replaced by a hydrogen, a fluorine, or a methyl group. The hydrogen-substituted dC analogue was converted into a 2’,3’-dideoxynucleoside, which was converted into a 5’-triphosphate derivative. The other two dC analogues were transformed into 5’-triphosphate derivatives immediately after Heck coupling reactions. These analogues will allow an examination of the nature and role of minor groove interactions betwee

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3

Sullivan, Shannon M. "Synthesis of 2,4-disubstituted pyrimidine derivatives as potential 5-HT7 receptor antagonist." unrestricted, 2008. http://etd.gsu.edu/theses/available/etd-05052008-153400/.

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Thesis (M.S.)--Georgia State University, 2008.<br>Title from file title page. Lucjan Strekowski, committee chair; A.L. Baumstark, Gabor Patonay, Doyle Barrow , committee members. Electronic text (68 p. : ill.) : digital, PDF file. Description based on contents viewed June 23, 2008. Includes bibliographical references (p. 42-430.

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4

Sūdžius, Jurgis. "Synthesis And Properties Of Pyrimidine Derivatives – Potent Carbonic Anhydrase Inhibitors." Doctoral thesis, Lithuanian Academic Libraries Network (LABT), 2011. http://vddb.laba.lt/obj/LT-eLABa-0001:E.02~2011~D_20110519_082332-05105.

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The aim of the work was design of pyrimidine derivatives – potent carbonic anhydrase (CA) inhibitors. Theoretical investigation of interaction of 4-[N-(pyrimidin-4-yl)]aminobenzenesulfonamides containing substituents at 2-, 5- and 6- positions of pyrimidine ring with an active site of hCAs suggested that these compounds can fit into an active site of the enzymes and should interact with them as typical hCA inhibitors. Synthesis of target compounds was carried out by substitution of chloro group at 4,6-dichloropyrimidines containing cyano-, formyl- or nitro groups at position 5 of the pyrimidin

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5

Taleli, Lebusetsa. "Radiosynthesis of various pyrimidine derivatives and determining their uptake into cells." Thesis, Cape Peninsula University of Technology, 2009. http://hdl.handle.net/20.500.11838/744.

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Thesis (MTech (Chemistry))--Cape Peninsula University of Technology, 2009<br>N3-substituted pyrimidine nucleoside derivatives containing either an iodovinyl moiety or an allyl group, i.e. [121]-N3-(3-iodoprop-2-en- l -yl)thymidine, (1~-711 and e21]-N3-(prop-2-enl- yl)-5-iodo-Z'-deoxyuridine, (1~_10, were synthesised and preliminarily evaluated by determining their uptake into CHO-Kl cells. Compound e~-711 was designed to be a delivery vector of 121: into the DNA of the cells, while (1~_10 was designed to serve as a control. Compound (1231]-711 was also intended to have a higher metabolic

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6

Weiss, Jason Thomas. "Development and application of bioorthogonal palladium-labile derivatives of cytotoxic pyrimidine analogues." Thesis, University of Edinburgh, 2015. http://hdl.handle.net/1842/15957.

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Chemotherapy is widely used to treat various forms of cancer. However, some chemotherapeutic drugs, due to their antineoplastic properties, also act upon healthy cells which normally replicate rapidly causing a plethora of undesirable side effects. One rising and promising therapeutic strategy is the development of prodrugs. Prodrugs are derivatives of the pharmaceutically active drugs but require an enzymatic or biochemical transformation within a certain biological space in order for it to become activated and capable of exerting the desired pharmacological effect. As a novel prodrug approac

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7

Li, Jiyang [Verfasser]. "Investigation of Phthalazine, Quinazoline and Pyrimidine Derivatives as ABCG2 Inhibitors / Jiyang Li." Bonn : Universitäts- und Landesbibliothek Bonn, 2018. http://d-nb.info/1167857135/34.

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8

Howie, Colin. "The design, synthesis and testing of hydantoin derivatives as inhibitors of pyrimidine biosynthesis." Thesis, University of Glasgow, 1989. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.278514.

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9

Rango, Enrico. "PRECLINICAL CHARACTERIZATION OF SFK INHIBITORS, PYRAZOLO[3,4-d]PYRIMIDINE SCAFFOLD-BASED DERIVATIVES, FOR CANCER TREATMENT." Doctoral thesis, Università di Siena, 2021. http://hdl.handle.net/11365/1140389.

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The first part of this thesis essentially focuses on the preclinical characterization of Si306, a pyrazolo[3,4-d]pyrimidine derivative, identified as a very promising anticancer agent. This compound has shown a favorable in vitro and in vivo activity profile against neuroblastoma (NB) and glioblastoma (GBM) models by acting as a competitive inhibitor of c-Src tyrosine kinase. Nevertheless, the good antitumor activity of Si306 is associated with sub-optimal aqueous solubility, which might hinder its further development. In this context, drug delivery systems were developed to overcome the poor

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10

GIACCHELLO, ILARIA. "Synthesis of properly substituted pyridine and pyrimidine derivatives and their biological evaluation as potential antiviral agents." Doctoral thesis, Università degli studi di Genova, 2019. http://hdl.handle.net/11567/940944.

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Influenza A viruses (IAVs) belong to the Orthomixoviridae, a family of enveloped viruses with a single-stranded negative-sense and eight-segmented RNA genome. They are the most prevalent pathogens for both humans and animals, causing the so-called seasonal flu and widespread pandemics. A part from the use of vaccines, viral infections can be inhibited at several crucial steps by the use of antiviral agents. It is possible to have an antiviral effect both targeting important proteins for the virus life cycle and targeting host proteins that play crucial roles during influenza virus infection. R

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11

Turner, Isabelle. "The study of ß-cyclodextrin interactions with sugars using inhibition kinetics and the bromination of pyrimidine derivatives." Thesis, National Library of Canada = Bibliothèque nationale du Canada, 1999. http://www.collectionscanada.ca/obj/s4/f2/dsk1/tape7/PQDD_0001/MQ43636.pdf.

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12

Gilliam, Sarah Elizabeth. "The mode of action and therapeutic potential of purine and pyrimidine phosphonylmethoxyalkyl derivatives against bovine herpesvirus-1." Thesis, University of Cambridge, 1992. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.319534.

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13

GRECO, CHIARA. "Synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine derivatives active as SGK1, Fyn and Src kinases inhibitors." Doctoral thesis, Università degli studi di Genova, 2020. http://hdl.handle.net/11567/1001600.

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The pathogenesis of many cancers is characterized by mutations, overexpression and dysregulation of protein kinases. As a result, increasing attention has been directed towards the identification of novel kinase inhibitors for cancer therapy. The work performed here focuses on the synthesis of a series of pyrazolo[3,4-d]pyrimidine derivatives as inhibitors of the serine-threonine kinase SGK1, and the tyrosine kinases Fyn and Src. The first set of compounds are analogues of the in house SGK1 inhibitor SI113 which had previously demonstrated anti-cancer activity. In fact SI113 resulted to b

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14

Girault, Isabelle. "Identification et dosage immunologique de lésions de l'ADN." Grenoble 1, 1995. http://www.theses.fr/1995GRE10123.

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Divers facteurs (agents oxydants, rayonnements) peuvent engendrer des modifications de bases de l'adn. Le premier volet de ce travail de these a consiste a identifier les produits de degradation des bases pyrimidiques par l'ozone. L'identification de ces composes a permis de mettre en evidence deux nouveaux derives et de conclure a un mecanisme d'action specifique. La suite du travail concerne la preparation d'anticorps diriges contre des modifications de bases de l'adn. Nous avons mis au point une nouvelle methode de preparation des antigenes destines a la production d'anticorps utilises pour

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15

Дербисбекова, У. Б., У. М. Датхаев, С. Е. Момбеков, К. Д. Рахимов, А. К. Шарапатдин та А. К. Шалабай. "Изучение острой и подострой токсичности субстанции с противогрибковым действием". Thesis, Сумский государственный университет, 2017. http://essuir.sumdu.edu.ua/handle/123456789/63259.

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В данной работе авторами исследована острая и подострая токсичность субстанции 2-(6-гидроксиметил-9-метил-2-(4-фторфенил)-5Н- пиридо[4',3':5,6]пирано[2,3-d]пиримидин-4-илсульфанил)-1-N- пиперидинилэтанона (производные 4Н-пиридо[4',3':5,6]пирано[2,3-d]пиримидина). Целью изучения острой и подострой токсичности субстанции является определение переносимых, токсических и летальных доз лекарственного средства и причин наступления гибели животных. Острую токсичность исследуемой субстанции изучали на белых беспородных мышах. Суспензию вводили животным однократно в желудок с помощью зонда в диа

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16

Borssum, Waalkes Marjan van. "Lipophilic derivatives of 5-fluoro-2'-deoxyuridine as liposomal anticancer agents." [S.l. : [Groningen : s.n.] ; University Library Groningen] [Host], 1992. http://irs.ub.rug.nl/ppn/292987617.

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17

Vieira, Andreia Sofia da Costa. "Rethinking Triazoles as Antifungals: Synthesis and Evaluation of New Triazole Derivatives." Master's thesis, Universidade Nova de Lisboa, Instituto de Tecnologia Química e Biológica António Xavier, 2017. http://hdl.handle.net/10362/81407.

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"In the last decades, fungal infections have become a serious problem, mainly due to the excessive use of this reduced number of drugs, leading to an increase of acquired resistances1. Therefore, it is urgent to develop new and more effective antifungal medicines. The main objective of this master's thesis was the development of novel antifungal drugs, based on triazoles and pyrimidines, combining two groups with antifungal properties, known to be active in combinatorial therapies, in a single molecule. For the synthesis of these compounds, Huisgen's 1,3-dipolar cycloaddition methodologies, c

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18

Rostamizadeh, S., N. Shadjou, and E. Isapoor. "MCM-41-nPrNH2 as a Recoverable Nanocatalyst for the Synthesis of New Phenylpyrido[4,3-d]pyrimidin-2-amine Derivatives." Thesis, Sumy State University, 2012. http://essuir.sumdu.edu.ua/handle/123456789/35002.

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MCM-41 anchored n-propylamine (MCM-41-nPrNH2) was found to be a highly efficient and recoverable nanocatalyst for the synthesis of new class of phenylpyrido[4,3-d]pyrimidin-2-amine derivatives under solvent free conditions in high to quantitative yields. All the structures of title compounds 3a-j were elucidated by comprehensive 1H NMR, 13C NMR, IR and Mass spectra When you are citing the document, use the following link http://essuir.sumdu.edu.ua/handle/123456789/35002

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19

Arellano, Michel. "Cardiotoxicité du 5-fluorouracile, médicament antitumoral majeur : mise en cause de la formulation et de la métabolisation." Toulouse 3, 1995. http://www.theses.fr/1995TOU30228.

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Le 5-fluorouracile (fu) est un des medicaments anticancereux les plus utilises dans le monde. Comme tous les cytostatiques, il presente des effets secondaires toxiques, en particulier hematologiques et digestifs, mais aussi neurologiques et cardiologiques. La cardiotoxicite observee chez certains patients traites au fu est en partie due a la presence d'impuretes fluorees presentes dans les solutions commerciales de fu. Ces impuretes sont en fait des produits de degradation du fu qui se forment avec le temps dans le milieu basique indispensable a la solubilisation de ce principe actif. Grace au

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20

Zhan, Wang Ming, and 王明仁. "Synthesis of disperse dyes from pyrimidine derivatives." Thesis, 1998. http://ndltd.ncl.edu.tw/handle/80617404323144404283.

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碩士<br>國立臺灣科技大學<br>纖維及高分子研究所<br>86<br>The pyrimidine derivatives were prepared by the reaction of malonic acid with urea or Thiocarbamine derivative. The condensation reaction of pyrimidine intermediates with aromatic aldehyde 、p-methoxycinnamaldehyde and 1,3,3-trimethyl-2-methylene indoline led to obtain three series of mono、di- and poly-methine pyrimidine disperse dyes, respectively. The structure of the dyes was confirmed by E.A,IR,MS and 1H- NMR spectral analysis.

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21

Chen, Tsai Pi, and 蔡弼丞. "Synthesis and Characterization of pyrazolo[1,5-a] Pyrimidine Derivatives." Thesis, 2004. http://ndltd.ncl.edu.tw/handle/73267789211679603689.

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碩士<br>國立臺灣科技大學<br>高分子工程系<br>92<br>ABSTRACT In this study, 4-arylazo-3,5-diaminopyrazole compounds have been synthesized by reaction of arylazomalononitrile with hydrazine hydrate. The symmetrical and asymmetrical 3,6-diarylazo-2,5,7- triaminopyrazolo[1,5-a]pyrimidine heterocyclic disazo dyes have been prepared by the cyclization of 4-arylazo-3,5-diaminopyrazoles with different arylazomalononitriles. The solvatochromic behaviour of these disazo dyes in various solvents was evaluated. The structures of these compounds were determined by spectrometry（UV、FT-IR、1H-NMR）and element analys

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22

張源杰. "Studies on pyrimidine derivatives and Schiff’s base complexes liquid crystals." Thesis, 2002. http://ndltd.ncl.edu.tw/handle/64962489648418360070.

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碩士<br>國立臺灣大學<br>化學研究所<br>90<br>Liquid crystalline base on Liquid crystal Display. Liquid crystal has the mesomorphic properties that become very hot investigated domain. Two types of liquid crystalline molecules have been investigated:(1) 2,4,6-triarylpyrimidine-based organic discotic liquid crystal. (2) Schiff’s base-derived rod-like liquid crystals. pyrimidine derivatives investigated result: Side chain length can made pyrimidine derivatives that has been 6 side chains and hexyloxyl side chain has liquid crystal properties. If alkoxy side chains was butyloxyl side chain, Pyrim

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23

Hsu, Chan Jung, and 許展榕. "Synthesis and Dyeing Properties of Aza-methine Dyes from Pyrimidine Derivatives." Thesis, 2000. http://ndltd.ncl.edu.tw/handle/19408498767026243071.

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碩士<br>國立臺灣科技大學<br>纖維及高分子工程研究所<br>88<br>Abstract The pyrimidine derivatives were prepared by the reaction of Malonic acid with urea in acetic anhydride. The pyrimidines reached with sodium nitrite to produced the Nitroso pyrimidines. The Aza-methine dyes were synthesised from the reaction of nitroso pyrimidinetrione with 1,3,3-trimethyl-2-methyene-indoline derivatives and the some pyridone derivatives , respectively. The structure of the dyes were confirmed by E.A、IR、MS 、1H-NMR and spectral analysis. The solvent effect in CHCl3 and DMSO were studied.

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24

LIOU, AN-SYUN, and 劉安訓. "Design and Synthesis of Pyrrolo[3,2-d]pyrimidine-based Derivatives as Potential Agents for Alzheimer’s Disease." Thesis, 2019. http://ndltd.ncl.edu.tw/handle/twum5f.

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25

Turner, Isabelle. "The study of Ý-cyclodextrin interactions with sugars using "inhibition kinetics" and the bromination of pyrimidine derivatives." Thesis, 1999. http://spectrum.library.concordia.ca/857/1/MQ43636.pdf.

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Part I . The binding of Ý-cyclodextrin (Ý-CD) with sugars was studied using "inhibition kinetics". The rates of hydrolysis of trimethyl orthobenzoate and benzaldehyde dimethyl acetal in acidic solution were monitored using a single beam stopped-flow spectrophotometer. Both substrates exhibit saturation kinetics and 1:1 binding with Ý-CD, and the rates of hydrolysis are retarded by the cyclodextrin, in agreement with earlier studies. The retarded rates of hydrolysis in the presence of Ý-CD are modulated by the addition of guests that bind to the CD, and "inhibition constants" (K 1 ) may be dete

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26

Lin, Yang-Chu, and 林洋鉅. "Studies on liquid crystals : Syntheses of Schiff''s base complexes with fluorinated side-chain , pyrimidine and triazine derivatives." Thesis, 2000. http://ndltd.ncl.edu.tw/handle/79173137596257102221.

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碩士<br>國立臺灣大學<br>化學研究所<br>88<br>We have introduced the perfluorinated aliphatic side chains into several Schiff''s base-typed liquid crystalline complexes and investigated the effects of fluorination on the mesophases. In general, the melting points of the perfluorinated complexes are higher than the corresponding hydrocarbon analogues, and the difference increases as increasing the number of the difluorine methylene units. Moreover, it was found that the introduction of the perfluorinated side chains stabilizes the Smetic phase in the SBL-3A-R series, but it inhibits the formation of the Sc ph

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27

Mohamed, Tarek. "Design, Synthesis and Biological Evaluation of 2,4-Disubstituted Pyrimidine Derivatives: Multifunctional Candidates as Potential Treatment Options for Alzheimer’s Disease." Thesis, 2011. http://hdl.handle.net/10012/6183.

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Alzheimer’s disease (AD) is a highly complex and rapidly progressive neurodegenerative disorder characterized by the systemic collapse of cognitive function and formation of dense amyloid-β (Aβ) plaques and neurofibrillary tangles (NFTs). AD pathology is derived from the cholinergic, amyloid and tau hypotheses, respectively. Current pharmacotherapy with known anti-cholinesterases, such as Aricept ® and Exelon ®, only offer symptomatic relief without any disease-modifying effects (DMEs). It is now clear that in order to prevent the rapid progression of AD, new therapeutic treatments should targ

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28

Tsai, Pi-Chen, and 蔡弼丞. "Synthesis and Solvatochromic Properties of Some Novel Symmetrical and Asymmetrical Heterocyclic Disazo Dyes Based on Pyrazolo[1,5-a]Pyrimidine Derivatives." Thesis, 2007. http://ndltd.ncl.edu.tw/handle/49g7pn.

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博士<br>國立臺灣科技大學<br>高分子系<br>95<br>The disertation consists of two main themes: Firstiy, (1) 3,5-Di-(amino or methyl)-4-substituted-azoly-pyrazole and 3-amino-5- methyl-4-substituted-azoly-pyrazole have been synthesized via the cyclization from hydrazine hydrate with 2-substituted-azoly-malono- nitrile, 3-sub-stituted-azoly-pentane-2,4-dione and 3-imino-2-substitu- ted-azoly-butyronitrile, respectively; and (2) 5-amino-3-methyl-4-substi -tuted-azoly-pyrazole and 3-amino-4-substituted-azoly-5-pyrazolone were prepared by coupling reaction of aniline derivatives with 3-amino-5-pyrazolone and 5-amino

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29

Changunda, Charles Reuben K. "Synthesis and evaluation of novel pyridine-, pyrimidine- and triazine-based derivatives as potential HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs)." Thesis, 2018. https://hdl.handle.net/10539/25741.

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A Dissertation submitted to the Faculty of Science, University of the Witwatersrand, in fulfilment of the requirements of the Doctor of Philosophy Johannesburg, 2018<br>As part of our goal to identify heterocyclic-based analogues that could act as allosteric inhibitors of the HIV-1 reverse transcriptase (RT) enzyme, small libraries of novel molecules containing pyridine, pyrimidine and triazine central cores were designed and synthesized for a preliminary in vitro assay against the wild-type RT virus. To achieve this goal, in the first instance we explored a scaffold-hopping approach as a pos

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30

Cardoso, Inês Sofia Soares Gomes Lains. "Design and synthesis of a novel pyrazolopyrimidine compound as a potential kinase inhibitor." Master's thesis, 2016. http://hdl.handle.net/10451/34606.

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Trabalho Final de Mestrado Integrado, Ciências Farmacêuticas, Universidade de Lisboa, Faculdade de Farmácia, 2016<br>Cancer is a generic term for a group of diseases in which abnormal cells have a fast and uncontrolled growth and proliferation, invading neighbouring tissues and spreading to parts of the body different from where it started. Cancer is placed second at the most important causes of death and morbidity in Europe and accounts for 1 in every 7 deaths worldwide, which is more than HIV, tuberculosis and malaria combined. Furthermore, the number of new cases worldwide is expected to r

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31

Chang, Chun-Hsi, and 張濬璽. "The study of selective synthesis and biological activity of pyrazolo[3,4-d]pyrimidine, N-(1H-pyrazol-5-yl)formamide, or N-(1H-pyrazol-5-yl)formamidine derivatives from N-1-Substituted-5-aminopyrazoles with new Vilsmeier-type reagents." Thesis, 2013. http://ndltd.ncl.edu.tw/handle/95634777776867134802.

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碩士<br>中國醫藥大學<br>藥物化學研究所碩士班<br>102<br>Various halomethyleniminium salts as novel Vilsmeier reagents were synthesized from the reaction of formamide or N-methylformamide with phosphoryl chloride. Treatment of N-1-substituted-aminopyrazoles including, N-1-(2-pyridinyl)-5-aminopyrazoles and N-1-(2-quinolinyl)-5-aminopyrazoles with these Vilsmeier reagents to obtain the corresponding pyrazolo[3,4-d]pyrimidine, N-(1H-pyrazol-5-yl)formamide, or N-(1H-pyrazol-5-yl)formamidine products. The experimentant results were different with our previous data which the formylated amidylpyazole and formamidine pr

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32

Wu, Yong-yi, and 吳永逸. "Studies on anti-cancer activity and molecular marker of 5-substituted 2-cyanoimino-4-imidazodinone and 2-cyanoimino-4- pyrimidinone derivatives based on xenograft lung carcinoma histoculture and animal model via injecting cancer cells into tail vein." Thesis, 2006. http://ndltd.ncl.edu.tw/handle/24532567461880611548.

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碩士<br>南台科技大學<br>生物科技系<br>94<br>Our present study aimed at evaluating putative possibility of using xenograft carcinoma as a model system to monitor effect of chemotherapy regiment of lung cancer. A series of novel synthesized, eg. 5-substituted 2-cyanoimino-4-imidazodinone and 2-cyanoimino-4-pyrimidinone derivative of compounds have been synthesized as anticancer agents. The derivatives exhibited cytotoxicity against a variety of lung cancer cell lines (LL2 and A549) were evaluated in MTS assay and the cell cycle population using flow cytometry assay. In addition, xenograft nude mice model

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