Global ETD Search
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 12 of 12 for “"Pro-Drugs"”.
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The design and synthesis of novel pro-drugs for the treatment of nephropathic cystinosis.
… compliance. In an attempt to overcome these problems, a number of pro-drug derivatives of cysteamine and cystamine, the disulfide analogue of cysteamine, have been synthesised and evaluated. Pro-drugs were synthesised using a route established in our laboratories. Briefly, cystamine …
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Probing Proteasome Inhibition By Metal Copmplexes As A New Route For Anticancer Therapy
… characterization. The antineoplastic properties of these metal-containing pro-drugs are tested against the inhibition activity of the 26S proteasome. Selected metal ions ranging from transition to main group elements have been incorporated in various ligand systems containing phenolate …
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Bioactivities of Antiestrogens and Antiestrogen Metabolites in the Rat and Mouse
… of the triarylethylene-type antiestrogens act as pro-drugs, being converted in vivo to metabolites having greater estrogenic and antiestrogenic potency than their parent compounds. This laboratory has revealed that two potent nonsteroidal antiestrogens,
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Two-Photon Microscopy of E-Combretastatin uptake and activation in live mammalian cells
… are powerful anticancer drugs that are being evaluated in phase I/II clinicaltrials. Combretastatins act by binding to p-tubulin, preventing microtubule assembly andinhibiting angiogenesis in developing tumours. Most widely studied is the natural …
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Synthesis and evaluation of novel antivascular agents for two-photon activation
… Combretastatins are powerful anticancer drugs with some derivatives in advanced clinical trials for cancer therapy. Combretastatins are stilbenes isolated from the African shrub Combretum caffrum. These agents interact with tubulin in a similar way to colchicine, causing destruction of …
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Kinetic studies of the hydrolysis reactions of ruthenium (III) complexes hIm trans-[RuCl₄(im)₂] and hInd trans-[RUCl₄(ind)₂] by uv-visible spectrophotometry
… <p>Ruthenium complexes are considered as pro-drugs, as they transform into antitumor active species in the body by hydrolysis, redox reactions, and reactions with biologically occurring nucleophiles. My project involved the synthesis of two ruthenium complexes with different ligands and …
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Photoresponsive nanosystems for therapeutic applications
… oxygen (1O2) and nitric oxide (NO), by using appropriate photochemical precursors represents a fascinating and unconventional approach for the treatment of cancerous and microbial diseases in non-invasive manner. However, many precursors have a hydrophobic nature, which favors their aggregation …
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Nitroaromatic pro-drug activation and resistance in the African trypanosome
… sickness. These compounds are believed to act as pro-drugs that require intracellular enzymatic activation for antimicrobial activity. Here, the role of the bacterial-like nitroreductase TbNTR as a nitrodrug activating enzyme is examined through overexpression and knock-out studies in T. brucei. …
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Behavioral and Neurochemical Characterization of the Effects of the Novel Adenosine Antogonist MSX-4
… to regulate such effort-related choice behavior processes. For instance, DA-R antagonists as well as NAc DA depletion can decrease choice behavior. Moreover, previous studies have shown that systemic administration of adenosine A<sub>2A</sub> antagonists reverses the behavioral effects of DA-R D2 …
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Analogues of Nitrofuran Antibiotics are Potent GroEL/ES Pro-drug Inhibitors with Efficacy against Enterococcus Faecium, Staphylococcus Aureus, and Escherichia Coli
… World Health Organization as some of the most prominent threats to human health, capable of developing significant antibiotic resistance. These pathogens contribute to over 2 million annual infections and ~23,000 annual deaths in the U.S. In addition, various strains of E. coli have also shown …
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Human Mesenchymal Stem Cell Homing to Glioma Stem Cell Xenografts
… primary brain tumor with a median survival of approximately one year. The current standard of care for GBM includes the maximal surgical resection, followed by concurrent chemotherapy, radiotherapy, and in some cases and adjuvant chemotherapy. Yet, despite this aggressive multimodal approach, GBM …
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Investigation of azithromycin analogues and proteasome-like inhibitors as quick-killing antimalarials
… cycle (2 days) via an unidentified mechanism, proposed to be independent of delayed death. Thus, we hypothesised that azithromycin could be redeveloped into an antimalarial with two different mechanisms of action against parasites: delayed death and quick-killing. Over 100 azithromycin …