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Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 16 of 16 for “"Quinazoline"”.
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New quinazoline analogues as NF-κB activation inhibitors
… We designed a series of compounds based on quinazoline scaffold pharmacophore model which may have high binding affinity with p50 subunit of NF-κB. The compound series with phenyl substitution at position 2 of quinazoline proved to be more effective at inhibiting NF-κB function both …
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Syntheses of Dimensionally Altered Enzyme Substrates by Means of the Finkelstein Reaction (Benzopurine, Naphthopurine)
… for the synthesis of 9-aminobenzimidazo{5,6-g}quinazoline (lin-naphthoadenine) and 9-amino-3-(beta)-D-ribofuranosylbenzimidazo{5,6-g}quinazoline (lin-naphthoadenosine) have been developed. The synthetic route commenced with 5,6-dimethylbenzimidazole and the linear array of rings was constructed …
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Computer-aided drug design and the biological evaluation of anti-cancer drugs
… to 6-amino-4-(4-phenoxyphenylethylamino) quinazoline, a potent inhibitor of the Nuclear Factor kappa B (NF-κB), a transcription factor that has a pivotal role in cancer survival and Pentamidine, an anti-parasitic drug that has recently been demonstrated to possess tumour-killing activity. …
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Design and synthesis of novel non peptidomimtic beta-secretase inhibitors in the treatment of Alzheimer's disease
… was replaced by 4-amino-quinoline or 4-amino-quinazoline rings. All the synthesized compounds were also evaluated in a modified FRET enzymatic assay (test B), changing the fluorescent substrate for enzymatic BACE1 cleavage. This test method guided deep structure-activity relationships for …
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Synthesis and SAR investigation of haemozoin-inhibiting quinazolines active against Plasmodium falciparum
… of a biologically relevant scaffold, 2,4-diaminoquinazoline, based on hits found by high-throughput screening were rationally designed and synthesised using a three-step procedure. This involved chlorination of benzoylene urea (1), followed by two successive nucleophilic aromatic substitution …
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The Discovery and Synthesis of Novel DYRK1A Inhibitors for Various Oncologic Targets
… Blastoma Multiforme (GBM) based “6,6 Aryl-Pip” quinazoline based analogs. These compounds serendipitously inhibit key GBM relevant kinases as a novel approach to treat this specific cancer. A series of molecules were made and analyzed in revealing potential IND candidates and in vivo candidates …
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Molecular orbital calculations of the activities of a series of CNS drugs
… of methaqualone (2-methyl-3-o-tolyl-4(3H)-quinazoline). The indices which were computed were frontier electron densities, charge densities, E<sub>HOMO</sub>, E<sub>LUMO</sub>, the difference between E<sub>HOMO</sub> and E<sub>LUMO</sub>, the electrophilic superdelocalizabillty using only …
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Elucidating the Target and Selectivity of a Non-Small Cell Lung Cancer Toxin
… Here, we report the discovery of the quinazoline dione compound (QDC), a molecule that exhibits selective toxicity across 100 non-small cell lung cancer (NSCLC) lines. Using photoreactive probes, we found that the QDC targets mitochondrial Complex I. We investigated the selective …
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Defined Dimensional Alterations in Enzyme Substrates. Synthesis and Enzymatic Evaluation of Some Lin-Naphthopurines
… and benzimidazo{5,6-g}-6H,8H-quinazoline-7,9-dione 4.8 (ANGSTROM) laterally extended dimensional derivatives of hypoxanthine and xanthine. These compounds, lin-naphthohypoxanthine and lin-naphthoxanthine, exhibited intense fluorescence. lin-Naphthoxanthine was not oxidized to …
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Direct synthesis of pyridine and pyrimidine derivatives
… amides to the corresponding pyrimidine and quinazoline derivatives, respectively, is described. The process involves amide activation with 2-chloropyridine and trifluoromethanesulfonic anhydride followed by nitrile addition into the reactive intermediate and cycloisomerization. In situ …
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SYNTHETIC AND MECHANISTIC STUDIES OF PRECIOUS METAL-MODIFIED TYROSINE KINASE INHIBITORS
… this, thiourea-modified 3-chloro-4-fluoroanilino-quinazoline derivatives were first studied as epidermal growth factor receptor (EGFR) tyrosine kinase-targeted carrier ligands in linear gold(I) complexes. The molecules mimic the EGFR inhibitor gefitinib. Gold(I) complexes were generated using …
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Design and Synthesis of Pyrimidine Based Heterocycles as Potential Anti-cancer Agents with Combination Chemotherapeutic Potential or Targeted One Carbon Metabolism Inhibition and Anti-opportunistic Agents
… cell resistance.</p> <p>Synthesis of substituted quinazoline and pyrido[3,2-<em>d</em>]pyrimidines is described. It also reviews the synthesis of multi-transporter (PCFT and FR) selective 5-substituted pyrrolo[2,3-<em>d</em>]/[3,2-<em>d</em>]pyrimidines as targeted one-carbon metabolism enzymes …
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Developments in Nickel-catalyzed Transfer Hydrocyanation Reactions and Novel Skeletal Editing Strategies through Nitrogen Atom Insertion
… including the transformation of indoles into quinazolines or quinoxalines, as well as pyrroles into pyrimidines, indenes into isoquinolines, or cyclopentadienes into pyridines (see Scheme II). The initial reaction design was based on the mechanistic proposal for the previously established …
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Structure-based development of novel chemical scaffolds as inhibitors of the store-operated calcium entry pathway
… composed of methylpyrazole ring bound to quinazoline and piperazine rings to have greater efficacy for SOCE inhibition. To conclude, a novel SOCE inhibitory scaffold with reasonable potency was identified through a structure-guided in silico screening campaign using hOrai1 homology model. …
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A mechanistic assessment of novel anticancer drugs targeting the metastatic cascade and tumour vascularisation.
… in this thesis are derived from the synthetic quinazoline derivate Verubulin or the natural drug Combretastatin A-4 (CA-4). Their preclinical evaluation includes the determination of their in vitro cytotoxicity profile against a panel of different tumour cells lines and various biochemical and …