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 17 of 17 for “"Anticancer therapeutics"”.
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Non-Neuroleptic Antitubercular and Anticancer Therapeutics through Rational Drug Remodelling of Phenothiazines and Related Antipsychotics
… phenothiazines hold promise as novel classes of therapeutics in other indications. However, in addition to inherent neuroleptic properties, phenothiazines and related antipsychotics elicit adverse side effects at clinically relevant doses thus precluding their extensive clinical application. …
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Synthetic Methodology and Application of Enamine [2+2] Cyclisations for Cyclobutane Synthesis. Development of Integrin Antagonists as Anticancer Therapeutics Towards a Total Synthesis of Providencin
Cyclobutanes represent an underutilised structural feature in medicinal chemistry, partially due to difficulties in forming them in an easy and controlled manner. Herein is described their application to a drug discovery project and development of the enamine [2+2] cyclisation; a straightforward …
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Development and Evaluation of Organometallic Anticancer Drug Candidates
There is an urgent need to find novel anticancer therapeutics with different mechanisms of action than platinum-containing drugs, particularly for patients who relapse after having been initially treated with a platinum-containing chemotherapy regimen. This chemoresistance phenomena, along with the …
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Development and Evaluation of Organometallic Anticancer Drug Candidates
There is an urgent need to find novel anticancer therapeutics with different mechanisms of action than platinum-containing drugs, particularly for patients who relapse after having been initially treated with a platinum-containing chemotherapy regimen. This chemoresistance phenomena, along with the …
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Synthesis and Antiproliferative Activity of C3' and B-ring Modified Paclitaxel Analogs
… contributions in supplying the arsenal of anticancer therapeutics, and was FDA approved for clinical use in 1992. In order to design simplified analogs, the conformation that paclitaxel adopts when binding to tubulin has been the subject of ongoing studies. Much evidence has led to a …
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Investigation of a Novel Formulation from Umbilical Cord Blood Stem Cell-Derived Exosomes and Antioxidant (Selenium) in Malignant Melanoma Cells
… are available or under investigation as anticancer therapeutics such as cell therapy, immunotherapy, gene therapy and nanotechnology-based strategies but they all have severe complications and side effects that limit their wider use. Methods: The present in vitro study has evaluated the …
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Investigation of a Novel Formulation from Umbilical Cord Blood Stem Cell-Derived Exosomes and Antioxidant (Selenium) in Malignant Melanoma Cells
… are available or under investigation as anticancer therapeutics such as cell therapy, immunotherapy, gene therapy and nanotechnology-based strategies but they all have severe complications and side effects that limit their wider use. Methods: The present in vitro study has evaluated the …
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NOVEL G-QUADRUPLEX BINDERS WITH POTENTIAL FOR A DUAL DNA CROSS-LINKING MECHANISM OF ACTION
… are of interest for development as potential anticancer therapeutics. Novel 10-oxoanthracene and substituted anthracenyl isoxazole esters (AIEs) were synthesized and characterized based on NMR studies. To date, quarfloxin is the only G-quadruplex ligand from the large number developed to …
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NOVEL G-QUADRUPLEX BINDERS WITH POTENTIAL FOR A DUAL DNA CROSS-LINKING MECHANISM OF ACTION
… are of interest for development as potential anticancer therapeutics. Novel 10-oxoanthracene and substituted anthracenyl isoxazole esters (AIEs) were synthesized and characterized based on NMR studies. To date, quarfloxin is the only G-quadruplex ligand from the large number developed to …
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Structural characterization of interaction of K11 and K63 mixed-linkage polyubiquitin chains with the tUIMs of epsin1
… information is crucial for the development of anticancer therapeutics targeting epsin1. The molecular basis for the linkage-specific recognition of K11 and K63 mixed-linkage polyubiquitin chains by the tandem UIMs of the endocytic adaptor protein epsin1 is investigated using a combination of …
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Strain-promoted Stapled Peptides for Inhibiting Protein-protein Interactions
… oncogenic p53 MDM2 PPI, a validated target for anticancer therapeutics. Three stapled peptides were found to have inhibitory activity, thus demonstrating the utility of the novel dialkynes in the preparation of PPI inhibitors. The functionalised stapled peptide formed from a meta-fluoro …
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Quantitative analysis of perivascular antibody distribution in solid tumors
… derived from them are an emerging class of anticancer therapeutics that have shown efficacy in a range of blood and solid tumors. Antibodies targeting solid tumors face considerable transport barriers in vivo, including blood clearance, extravasation, diffusion within the tumor interstitium, …
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Targeting Histone Deacetylases (Hdac) For The Treatment of Soft Tissue Sarcoma
… deactylase inhibitors (HDACi) are a new class of anticancer therapeutics; however, little is known about HDACi or the individual contribution of HDAC isoform activity in soft tissue sarcoma (STS). We investigated the potential efficacy of HDACi as monotherapy and in combination with chemotherapy …
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Targeted magnetic hyperthermia for lung cancer
… the potential for developing highly effective anticancer therapeutics through designed aggregation of SPIO nanoparticles. Cancer stem cells (CSCs) are a sub-population of stem-like cells that are thought to be responsible for tumor drug resistance and relapse. We determined the susceptibility …
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A study on the interactions of synthetic IGF-II analogues with the type 1 IGF and insulin receptors.
… the improved design and development of potential anticancer therapeutics. A crystal structure of IGF-II bound to either the IGF-1R or the IR-A has not been reported. Thus, the precise location of IGF-II within the receptor binding pocket remains undefined. A fluorescence resonance energy transfer …
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Procaspase-3 activation as a strategy to overcome resistance to targeted anticancer therapies
… in exploiting procaspase-3 overexpression as an anticancer strategy. In particular, I will outline the preclinical and clinical development of a selective procaspase-3 activating small molecule (PAC-1) as an anticancer therapy. Activation of an executioner caspase such as caspase-3 leads to …
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DEVELOPING CHEMICAL TOOLS TO MAP MOLECULAR MECHANISMS THAT DRIVE DISEASE
… health is of paramount importance in designing therapeutics that effectively prevent and treat disease, as well as discovering biomarkers which enable early detection. Despite immense research efforts from the scientific community, there is much remaining to learn about these microscopic …