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 “"Novel Small Molecules"”.
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Novel small molecules for modulation of bacterial signaling pathways
… an urgent need to develop new antibiotics and/or novel strategies that do not induce bacterial resistance. Bacteria employ a population-dependent cell-to-cell communication system known as quorum sensing (QS) to express various pathogenic traits such as virulence factor production and biofilm …
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Development and Mechanistic Characterization of Novel Small Molecules as Cancer Therapeutics
The discovery and development of novel small molecules as anti-cancer agents plays an integral role in the fight against cancer. Such efforts will lead to the development of the therapies of tomorrow. Potentially useful molecules may be discovered through cell-based toxicity screens, enzyme-based …
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Generation of novel small molecules as inhibitors of plasminogen activator inhibitor-1
… The goal of this research study is to design novel, potent, and specific small molecule inhibitors of PAI-1. The structural intricacy of the PAI-1 allows for multiple prospective binding sites. This research study explores the synthesis and screening of biological activity of various …
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Synthesis and structure activity relationship of novel small molecules as inhibitors of plasminogen activator inhibitor-1
… and impact of the different derivatives of those small molecules on PAI-1 inhibition.</p>
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Design, synthesis, and preliminary biological evaluation of novel small molecules modulating the HuR RNA-binding protein and other therapeutically relevant targets in immuno-oncology.
… advanced cancer development, my aim was to find novel small organic molecules to disrupt the mRNA-HuR interaction and act as cytotoxic agents. The second part of my Ph.D. thesis deals with two biological pathways related to cancer immunotherapy. PD-1 (Programmed Death receptor 1) – a type I …
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Design, synthesis and evaluation of small molecules as inhibitors of plasminogen activator inhibitor-1
… we describe the synthesis and evaluation of novel low molecular weight amides containing various moieties, including para-chlorobenzyl, polyphenol, oxindole, or isatin-based units. By changing the architectural scheme of these compounds we hope to effectively change the potency of our …
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Synthesis and modification of pamam dendrimers as histone replacement molecules
… molecular dynamic simulations. The synthesis of novel small molecules based around L-histidine and photo-responsive azobenzene, and the use of these to modify the surface of 4th and 5th generation PAMAM dendrimers is reported in Chapters 4 and 5 respectively. There follows a final chapter …
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Exploring the effects and efficacy of novel cell cycle regulating compounds in aggressive Breast, Ovarian and Cervical Cancer
… compounds and to test the cytotoxicity of three novel small molecules that interfere with cell cycle progression in cancer cells, ultimately inducing apoptosis (cell death). MTT and clonogenic assays were the techniques selected to test the cytotoxicity of the compounds in a cancer cell line …
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Functional Investigation of Dual αvβ3 and αllbβ3 Integrin Inhibition in Haematological and Solid Tumour Models
… of the known β3 antagonists. A panel of 12 novel small molecules developed in the ICT was investigated for cytotoxicity and activity in the validated function assays. ICT9055 was the most potent antagonist in inhibition of cell adhesion, migration, and inducing cell detachment. The data …
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Development and application of carbon-carbon bond forming methodologies
The construction of novel small molecules is an invaluable tool to the fields of chemical biology and drug discovery. Information gained from introducing unique chemical moieties to biological systems allows for a better understanding of the governing dynamics of cellular mechanisms leading to new …
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Glioma: A Tale of Corticosteroids, Thiopurines and Proposed Novel AntiGlioma Small Molecules
… assessed the anticancer activity of 2 classes of novel small molecules; tetrahydroisoquinoline (THIQ) and chromenes. These molecules were screened in vitro to find the most potent anticancer derivatives that exhibited the least toxicity on normal stromal cells. EDL-360 (5-10 µM) and SP-6-27 (IC50 …
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Small-molecule approaches to interrogate the druggability of the VHL E3 Cullin RING Ubiquitin Ligase
… recent progress has led to the discovery of small molecule modulators of PPIs as chemical probes or lead compounds that have entered clinical trials. These findings have motivated more drug discovery programs to target PPIs. E3 ubiquitin ligases are attractive targets within the ubiquitin …
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Targeting an E3 ubiquitin ligase Siah1 and a cysteine protease SENP1 using SPR and DSF-based fragment screening
… involve large surface areas, while SENP1 has a small active site, making it hard to identify ligands for these proteins. The fragment-based approach has emerged as a complementary method to high-throughput screening of finding novel small molecules. The main aim of the study was to examine …
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Towards the development of fluorescent probes targeting aldehyde dehydrogenase (ALDH) in cancer. Expression and epigenetic modulation of ALDH1A1, ALDH2 and ALDH3A1 in selected in vitro models.
… of stem cells (SCs). In this study, a library of novel small molecules (1,4-di-substituted acetalanthraquinones, AAQs), containing an acetal group as protected aldehyde functionality, was designed with the aim of probing affinity for ALDH metabolism and demonstrating their potential as molecular …
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Towards the development of fluorescent probes targeting aldehyde dehydrogenase (ALDH) in cancer. Expression and epigenetic modulation of ALDH1A1, ALDH2 and ALDH3A1 in selected in vitro models.
… of stem cells (SCs). In this study, a library of novel small molecules (1,4-di-substituted acetalanthraquinones, AAQs), containing an acetal group as protected aldehyde functionality, was designed with the aim of probing affinity for ALDH metabolism and demonstrating their potential as molecular …
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Targeting the Colchicine Binding Site on Tubulin to Overcome Multidrug Resistance and Anticancer Efficacy of Selective Survivin Inhibitors
… Herein, we evaluated the anticancer activity of novel small-molecules that target the colchicine binding site, focusing on the most promising compounds from several structural scaffolds including indolyl-imidazopyridines (DJ95 and DJ101), VERU-111 analogs with a modified indole moiety (10ab and …
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A chemical biology study of human embryonic stem cell pluripotency and differentiation
… pathways at the molecular and cellular level is small molecules. High-throughput screening (HTS) of combinatorial chemical libraries is widely used for the search of such bioactive small molecules. My dissertation has focused on using HTS to identify novel small molecules that regulate hESC …