RSS 1.0Pharmaceutical Chemistry (Theses and Dissertations)
Recent Submissions
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Circulating miRNA biomarkers in Metabolic Syndrome and clinical obesity and their link with triple negative breast cancer
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2017)Metabolic syndrome (MetS), which is a spectrum of conditions including abdominal obesity, dyslipidemia, hypertension, and insulin resistance are increasing in prevalence globally and lead to an increased risk of cardiovascular ... -
Investigations of mechanisms of drug-resistance and associated biomarkers in HER2-overexpressing breast cancer
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2016)Breast cancer is the most commonly diagnosed cancer amongst women in Ireland. HER2-overexpressing breast cancer accounts for 25-30% of all breast cancer cases and was the focus of this project. While treatment options for ... -
Studies into the in vitro metabolism and antiplatelet effects of novel aspirin ester prodrugs
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2003)Aspirin is the most commonly used antiplatelet agent in the world, and is invaluable in prevention o f myocardial infarction, thrombosis and stroke. However prolonged use has been associated with gastrointestinal side-effects ... -
Stability and hydrolysis studies of novel dual acting conjugate drugs with anitcancer activity
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2011)Tamoxifen is currently a first-line endocrine therapy for the adjuvant treatment of Estrogen Receptor (ER) positive breast cancer. The antiestrogenic properties of this compound are related to its ability to compete for ... -
The design, synthesis and biological evaluation of novel barbiturate-based MMP inhibitors
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2010)Matrix metalloproteinases (MMPs) are a group of Zn-dependent endopeptidases that participate in many diseases. Two MMPs, MMP-2 and MMP-9, which are especially associated with inflammatory diseases and tumor metastasis have ... -
Investigations of beta-lactams as novel bioactive compounds
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2013)A natural stilbene product combretastatin A-4 (CA-4) is a known anti-cancer compound, which exerts its mechanism of action at the colchicine binding site on tubulin, a protein that is essential for the replication of cells. ... -
Flexible estrogen receptor modulators
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2005)Tamoxifen is a selective estrogen receptor modulator (SERM) with a triarylethylene structure, which has estrogenic activity in bone and endometrial tissue, yet antagonises the actions of estrogen in other tissues including ... -
Characterisation and analysis of beta-aminoketones as potential prodrugs for amines
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2004)The aim of the work described in this thesis is to evaluate the potential of β-aminoketones as amine prodrugs. These compounds are usually stable in acidic conditions while they cleave into the parent amine and an ... -
Design and synthesis of 4-[1,3-diaryl-1H-pyrazole-4-yl]-2,6-dimethyl-1,4-dihydropyridine compounds and evaluation as anti-proliferative and multi-drug resistance reversal agents
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2012)1,4-Dihydropyridines are well known for their use as calcium channel blockers and are extensively used in treatment of hypertension. Dihydropyridine derivatives such as nifedipine have been shown to have the potential to ... -
The synthesis and biochemical evaluation of novel isoquinoline derivatives
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2005)Isoquinolines are naturally occurring alkaloids, some of which have pharmacological activity. Previous work by the research group of Dr. Mary Jane Meegan, has shown diverse classes of isoquinoline derivatives to be active ... -
Synthesis, biochemical evaluation and structural studies of novel antiproliferative βeta-lactams
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2010)The synthesis and antiproliferative evaluation of anti-cancer β-lactams targeting tubulin, heat shock protein 90 and the estrogen receptor is described. Compounds were planned to include relevant substituents known to ... -
Studies in the synthesis and in vitro hydrolysis of novel aspirin prodrugs
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2003)Prolonged aspirin use has been associated with an increased risk of gastrointestinal bleeding, leading in some instances to haemorrhage and death. This thesis describes the design of aspirin prodrugs, from which aspirin ... -
Design, synthesis and biochemical evaluation of novel antiproliferative agents for the treatement of Burkitt's Lymphoma
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2011)This thesis is concerned with the identification of novel antiproliferative agents for the treatment of Burkitt's lymphoma (BL), an aggressive B-cell malignancy. Numerous SERT and NET ligand such as SSRIs and TCAs, having ... -
The design, synthesis and biochemical evaluation of analogues of dehydroepiandrosterone (DHEA) and novel selective oestrogen receptor modulators (SERMs)
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2002)This thesis is presented in four sections. In the first section the synthesis of a series of B ring derivatives of dehydroepiandrosterone (DHEA) is described. DHEA is the most abundant steroid in human plasma and has been ... -
Development, validation and optimisation of a vHTS protocol for identification of estrogen receptor modulators
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2006)The discovery of small-molecule drugs has reached a critical point in time where the number of new drugs released to market has become static regardless of the technological advances observed over the last few years. ... -
Dual acting nuclear receptor targeting conjugates : design, synthesis and biochemical evaluation
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2013)Breast cancer has become the second most common cancer worldwide after lung cancer, the fifth most common cause of cancer death, and the foremost cause of cancer death in women. Worldwide, breast cancer exceeds all other ... -
Design, synthesis and biochemical evaluation of dual-acting, estrogen receptor ligand conjugates
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2008)Selective targeting of malignancies over healthy cells is an important goal in cancer therapies. Knowledge of environmental and biological differences between tumours and healthy tissue can present suitable targets for ... -
Studies in the synthesis and impurity profiling of Methylenedioxy and Alkylthioamphetamines
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2002)3,4-Methylenedioxymethamphetamme (MDMA, Ecstasy) and other, so-called, designer amphetamines, have become popular drugs of abuse over the past number of years. Detailed knowledge of the synthetic methods employed by ... -
Synthetic, photophysical and biological studies into new tools for investigating bile acid disposition and toxicity
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2013)The overall objective of this thesis was to use synthetic chemistry to provide tools to understand problems in bile acid research including their disposition and mechanism of toxicity. Fluorescent reporter groups are very ... -
The design, synthesis and biochemical evaluation of novel flexible and conformationally restrained antiestrogens
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2000)This thesis is presented in four different sections. In the first section the synthesis of a number of structural (novel flexible) analogues of the antiestrogen drug tamoxifen is described. Preparation of novel conformationally ...
