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Showing 1 to 20 of 26 for “"5-substituted"”.
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Modified Purines. Rearrangement Through 5-Substituted Purine Intermediates
… (1) which are analogues of N(9)-substituted guanines, hypoxanthines, and xanthines. Structures were established in this series (1) on the basis of precursors and routes of synthesis, infrared spectra, mass spectra, ('1)H and ('13)C nuclear magnetic resonance spectra, and X-ray …
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Synthesis of Novel 6-Substituted and 5-Substituted Pyrrolo[2,3-D] Pyrimidine Antifolates as Targeted Anticancer Therapies
… The design and synthesis of classical 6- substituted pyrrolo[2,3-<em>d</em>]pyrimidines and 5-substituted pyrrolo[2,3-<em>d</em>]pyrimidines as potential antifolates have been described. The design variations include: methylated thiophene regioisomers, fluorinated phenyl regioisomers, …
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Synthesis of novel 5-substituted pyrrolo[2,3-d]pyrimidine antifolates as selective and potent anti-tumor agents
… inside the tumor. Based on this premise, five 5-substituted pyrrolo[2,3-<em>d</em>]pyrimidines have been designed, synthesized and characterized. Among them four are novel compounds and one is a previously reported compound. The previously reported compound has never been tested for …
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Classical Antifolates: Synthesis of 5-Substituted, 6-Substituted and 7-Substituted Pyrrolo[2,3-d]Pyrimidines as Targeted Anticancer Therapies
… study, twelve series of classical 5-, 6- and 7-substituted pyrrolo[2, 3-d]pyrimidines were designed and synthesized. Extensive structure modifications of the pyrrolo[2, 3-d] pyrimidine scaffold were investigated to determine selective transport via FR or/and PCFT and tumor targeted antifolates …
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Design, synthesis, and evaluation of bioactive molecules; Chiral polyvinylpyrrolidones supported Cu/Au nanoclusters catalyzed cyclization of 5-substituted nona-1,8-dien-5-ols
… properties. Chapter 4 described chiral-substituted poly-N-vinylpyrrolidones (CSPVP) supported Cu/Au nanoclusters mediation of cyclization reaction of 5-substituted nona-1,8-dien-5-ols. A five-member cyclized lactone possessing a stereogenic tetrasubstituted carbon center was formed in a …
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Studies in the synthesis of pyrimidines, pyrazoles, and pyrazolo pyrimidines. New syntheses of 1, 3 and 5 substituted pyrazolo [3, 4-d] pyrimidines, including glycosides related to naturally occurring pyrimidines, imidazoles, purines and their nucleoside derivatives.
Some compounds, analogous to those found in naturally occurring systems, are found to possess chemotherapeutic activity. Some, in the form of their nucleoside or nucleotide derivatives, are valuable antimetabolites in that they may block normal RNA or DNA polymerisation, or may be incorporated into …
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Baltymų amiloidinės agregacijos slopinimui skirtų 5-pakeistų-7H-imidazo[2,1-b][1,3]tiazinų sintezė /
… thesis of Gintarė Sapežinskaitė “Synthesis of 5-Substituted-7H-imidazo[2,1-b][1,3]thiazines for Inhibition of Amyloid Aggregation” Supervisor doc. dr. Ieva Žutautė. Vilnius University Faculty of Medicine Institute of Biomedical Sciences Pharmacy and Pharmacology Center. Vilnius, 2024. Aim of …
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Discovery of Pyrimidine-based Heterocycles as Single Agents With Combination Chemotherapy Potential And As Inhibitors Of Purine Nucleotide Biosynthesis For The Treatment of Cancer
… also describes selective tumor targeting with 5-substituted pyrrolo[2,3-<em>d</em>]pyrimidines analogs with heteroatom bridge substitution<strong> </strong>as GARFTase inhibitors.<strong></strong></p> <p>The work in this dissertation is centered on identifying structural features that are …
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Synthesis and Complexation Studies of Heterocyclic Compounds With Two or Three Contiguous Hydrogen Bonding Sites
… synthetic methodology was developed to produce 5-substituted anthyridine analogs. These compounds exhibited increased stability over the unsubstituted anthyridines. A novel hydrogen bond donor-donor-acceptor (DDA) unit was synthesized to mimic the hydrogen bond functionality of guanosine. A …
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Synthesis and Coordination Studies of Novel Heteroaryl Tetrazoles
… coordination studies of an array of heteroaryl 5-substituted tetrazole ligands. A family of 5-substituted pyridyl tetrazole ligands with various functionalities tethered to the tetrazole moiety were prepared and fully characterised. These ligands were reacted with various MX2 salts (M = Cu, Ni, …
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Brønsted acid-catalyzed alkylation of tetrazoles with alcohols
… developed a methodology for the alkylation of 5-substituted tetrazoles with benzhydryl and benzylic alcohols in the presence of 5 mol% of a mild Brønsted acid catalyst HBF4 (aq). The developed protocol features low acid catalyst loading, short reaction times, generally high yields and high N2 …
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Synthesis and Spectroscopic Studies of Substituted Pyrrolocytidines
… in order to compare its properties with its 6-substituted pyrrolocytidine counterpart. Unfortunately, the 5-substituted pyrrolocytidine was not achieved. The synthesis of five nucleosides based on the pyrrolocytidine scaffold was reported. Their synthesis was achieved through the tandem …
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Aspects of the chemistry of 1,4-naphthoquinones. An investigation of nucleophilic substitution reactions of alkylamines and hydroxyalyklamines on 1,4 napthoquinones and the role of solvent on the position of substitution.
… alkylamines, and hydroxyalkylamines with 5-substituted-1,4-naphthoquinones have been studied. It has been found that the nature of the solvent employed in the reaction influences the position of mono-substitution at either the 2- or 3-position. Although both regioisomers were produced in all …
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6- and 5-Halodecaboranes: Selective Syntheses From ClOSO-B10H10(2-) and Use as Polyborane Building Blocks
… compounds were then isomerized to their 5-substituted isomers through base catalysis. The isomerization was driven by the energy differences between the anionic-forms of each respective isomer. These reactions provided 5-halodeboranes in high yields. The bridging-hydrogens of the …
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Design, Synthesis and Biological Evaluation of Novel Cannabinoid Antagonist
… receptor affinity for a series of 4,5-diaryl-1-substituted-1,2,3-triazoles of ester and ketones is described. These derivatives were synthesized via a one-pot regiospecific click/acylation reaction sequence from 1-azido-2,4-dichlorobenzene and commercially available arylacetylenes. From the …
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Messa a punto di procedure per la semi-sintesi di composti ad attività antitumorale partendo da prodotti naturali. Studi di struttura-attività
… here the semi-synthesis of a new family of 5-substituted CPT's, along with their biological activity evaluation, which will be compared with reference compounds. The use of carrier-linked prodrugs has emerged as a useful strategy to overcome some of the drawbacks related with the use of the …
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Πορείες συνθέσεως ενώσεων με βιολογικό ενδιαφέρον από 2Η-πυραν-3(6Η)-όνες
… iv) A convenient and high yield synthesis of 5-substituted 2-pyrrolidinon.es via 2H-pyran-3 (6H)-ones, via 2H-pyran3(6H)-ones. Part III contains the experimental procedures and references.
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The design, synthesis, and biological evaluation of aplysinopsin analogs as potential neuromodulators
… for 5-HT2B and 5-HT2C receptor subtypes. C-5 Substituted compounds (88 and 89) had potent and selective inhibitory activity at MAO-A. Compounds 83, 88, and 89 were evaluated in the chick-anxiety depression model to evaluate their in vivo efficacy. Compound 83 shomodest antidepressant activity …
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In silico-guided design, synthesis and antimicrobial activity of piperazine-linked 8-hydroxyquinoline-isatin hybrids
… 11. The Mannich reaction of unsubstituted/5- substituted isatin with 11, yielded Mannich bases 14a-c with yields ranging between 56 - 60%. Proposed structures of the novel hybrids, 14a-c were confirmed by means of infrared, 1H- and 13C-NMR spectroscopy. Antimicrobial activity …
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