Browsing Pharmaceutical Chemistry (Theses and Dissertations) by Title
Now showing items 11-25 of 25
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Identification of novel targets for cancer chemotherapeutic agents : design, synthesis and evaluation of chromene based compounds with affinity for steroid hormone receptors
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2013)Breast cancer is the second most common cancer in Ireland and accounts for 28% of all cancers in women in Ireland, with an average of 1726 new diagnosis each year. One of the major therapeutic advances in clinical treatment ... -
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. ... -
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 ... -
Studies in the design and synthesis of novel selective serotonin reuptake inhibitors
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2005)The serotonin transporter (SERT) has been the target of several modern day antidepressants with the focus on achieving selectivity over other monoamine transporters, thereby minimising the side effects observed in the older ... -
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 ... -
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 ... -
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 ... -
Synthesis of intermediates for carbapenem antibiotics and synthetic analogues of dehydroepiandrosterone (DHEA)
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2000)The work presented in this thesis is divided into two parts. Part one consists of the synthesis and chemical modification of β-lactams as potential intermediates for carbapenem antibiotics. Part two describes the synthesis ... -
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 ... -
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 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 ... -
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 ... -
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 ... -
The design, synthesis, and evaluation of the Azetidin-2-one ring as a scaffold for novel combretastatin A4 analogues
(Trinity College (Dublin, Ireland). School of Pharmacy & Pharmaceutical Sciences, 2009)Combretastatin A-4 (CA4) is a natural product first isolated from the Combretum caffrum South African willow tree by Pettit and co-workers. CA4 has proved to be a potent antimitotic agent, with a mechanism of action ... -
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 ...