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Medicinal-Pharmaceutical Chemistry Commons™
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Articles 1 - 11 of 11
Full-Text Articles in Medicinal-Pharmaceutical Chemistry
Assessment And Health Benefit Of Vitamin C Using A549 Cell, Yetunde Adepoju
Assessment And Health Benefit Of Vitamin C Using A549 Cell, Yetunde Adepoju
College of Graduate Studies: Theses & Dissertations
Vitamin C (ascorbic acid) is a vital micronutrient recognized for its antioxidant capacity and essential bodily functions, such as collagen formation, neurotransmitter activity, and regulation of the immune system. This study explores how vitamin C can protect and potentially heal cells under oxidative stress and inflammation, using A549 cells, a human lung epithelial cell line, as the model system. The cells were exposed to varying concentrations of vitamin C dissolved in water, DMSO, and 5% DMSO. To assess the outcome, cell viability was measured with an MTT assay. In addition, the expression of key genes related to oxidative stress and …
The Synthesis And Biocatalytic Reduction Of Beta-Keto Alkynes, Rhema M. Francis
The Synthesis And Biocatalytic Reduction Of Beta-Keto Alkynes, Rhema M. Francis
College of Graduate Studies: Theses & Dissertations
The preparation of enantiopure homopropargyl alcohols (but-3-yn-ols) is of high importance to the scientific community. They are employed as valuable pharmaceutical intermediates and are opportune to generate antiviral nucleoside analogues. Chiral inducement of these molecules thus far has been poor (low ee) and has constituted a key challenge for asymmetric synthesis in the last few decades. Enzyme-catalyzed enantioselective reductions of ketones have become popular to produce thus-prepared synthons on an industrial scale. Among them, biocatalysts (dehydrogenases, reductases) emerge as a biodegradable option for chemical transformations, in comparison to chiral catalysts that employ highly toxic metals. This research investigates the catalytic …
Structure Activity Relationship (Sar) Studies Of Neurotoxin Quinoline-Derivatives, Dylan Smeyne
Structure Activity Relationship (Sar) Studies Of Neurotoxin Quinoline-Derivatives, Dylan Smeyne
Honors College Theses
Structure activity relationship (SAR) studies are performed in order to identify the core structure that is responsible for the biological activity of an organic molecule. Recently, we have synthesized a drug prototype which contains several functional groups, such as an alcohol, an ester, a fluorine, and an aromatic ring. While studying in vivo toxicity of this molecule in zebrafish (Danio rerio) embryo, we observed that it has a unique biological activity that causes a sudden inactivity in embryo movement. Continued investigation revealed that this molecule blocks sodium channels in neurons causing a temporary anesthesia in Danio rerio embryo. The biological …
Synthesized Tripodal Amine As Potential Anti-Cancer Therapeutic, Abigail G. Mcnamee
Synthesized Tripodal Amine As Potential Anti-Cancer Therapeutic, Abigail G. Mcnamee
Honors College Theses
Cancer remains a prevalent disease today. This disease may manifest itself in many different ways and affect a variety of tissues with everything from the brain to the blood. With this wide diversity of cancer types, treatment can be complicated since there is not a “one size fits all” treatment for the disease. Surgery, radiation, and chemotherapy are all options that must be weighed with their benefits and side effects. Ultimately though, there are not enough effective treatment options available for every type of cancer. This leaves many with the grim prognosis of never being cured. With this clear need …
Synthesis And Biological Activity Of Novel Tu100 Derivatives, Oladotun J. Alao
Synthesis And Biological Activity Of Novel Tu100 Derivatives, Oladotun J. Alao
College of Graduate Studies: Theses & Dissertations
In an attempt to create more effective chemotherapeutic compounds, the naphthoquinone adduct, 12,13-dihydro-N-methyl-6,11,13-trioxo-5H-benzo[4,5]cyclohepta [1,2 b]naphthalen-5,12-imine (hereafter called TU100) was synthesized. Inspired by its unique and novel mechanism of action, a series of structural derivatives were synthesized to explore structure-activity relationships. The analogues exhibited different cytotoxicity profiles, revealing the indicated regions are involved in cell death induction. Furthermore, the analogues had dramatically different effects on cellular ATP production, suggesting different molecular targets. Synthesis, biological activity, and SAR study of these analogues will be revealed.
Synthesis Of Multifunctional Polyacrylates And A Binding Group To Hemoglobin For The Treatment Of Traumatic Brain Injuries, Marina Michaud
Synthesis Of Multifunctional Polyacrylates And A Binding Group To Hemoglobin For The Treatment Of Traumatic Brain Injuries, Marina Michaud
Honors College Theses
Hemoglobin based oxygen carriers (HBOCs) hold promise as an effective emergency treatment of severe traumatic brain injuries (TBI). In the latest generation of HBOCs, polynitroxyl-pegylated hemoglobin (PNPH), cell-free hemoglobin is modified with TEMPO and PEG which reduce the toxicities associated with earlier generations of HBOCs. In our efforts to optimize the economic and therapeutic impacts of PNPH’s we have synthesized polydimethylaminoethyl methacrylate (poly-DMAEMA) under controlled living conditions via reverse addition-fragmentation chain transfer (RAFT) polymerization. The poly-DMAEMA was then successfully functionalized via quaternization of its NMe2 groups using chloroacetate derivatives of the TEMPO and PEG. This process was quantitative and …
Investigation Of The Effects Of Ionic Interactions In Peptide And Protein Structure, Aimee Lorts
Investigation Of The Effects Of Ionic Interactions In Peptide And Protein Structure, Aimee Lorts
College of Graduate Studies: Theses & Dissertations
Proteins and their unique structures are important due to their involvement in every cellular task, but the protein can only function properly when it is in the correct fold. β-sheet peptides and collagen were observed via structural studies. Circular dichroism (CD) determines a protein’s secondary structure. WKWK, a beta-sheet peptide, is known to dissolve in aqueous solutions. However, WKWK was observed to precipitate out of deionized water. To investigate the cause of this precipitation, Inductively Coupled Plasma Mass Spectroscopy (ICP-MS) was used to determine the ion content of the water. Elevated sodium ion concentrations were found to disrupt the stabilizing …
Exploring The Relationship Of Mbd1 Protein Binding Cpg Sites Of Methylated Dna, Shelby L. Scherer
Exploring The Relationship Of Mbd1 Protein Binding Cpg Sites Of Methylated Dna, Shelby L. Scherer
Honors College Theses
Methylated DNA binding (MBD) proteins control transcriptional regulation by binding methylated DNA at CpG islands to modulate transcriptional activation and silencing of specific genes such as tumor suppressors. The goal is to explore the structure/function relationship between MBD proteins and methylated DNA recognition. By synthesizing the methylated DNA binding region of the MBD1 protein, binding studies test the peptide’s affinity and specificity for methylated DNA. Fluorescence, circular dichroism, and thermal denaturation techniques are utilized to determine the binding affinities and structures of peptides. Studies of peptide mutations can monitor the effectiveness of methylated DNA binding compared to the original peptide. …
The Study Of Nf-Κb Peptide Mimics And How Proteins Bind Dna, Allee M. Murray
The Study Of Nf-Κb Peptide Mimics And How Proteins Bind Dna, Allee M. Murray
Honors College Theses
The protein complex nuclear factor kappa B (NF-κB) is widely considered to be one of the most influential transcription factors when studying cellular functions. Peptide mimics of NF-κB aim to inhibit DNA binding in order to displace the natural transcription factor, therefore inhibiting transcription and translation. In theory, NF-κB is not the problem; the real problem lies in directing the synthesis and expression of harmful proteins. In conjunction with this, the project aims to study NF-κB and its structure and function to determine what criteria are important for the binding of DNA in order to design a peptide that comes …
The Synthesis And Biological Activity Of Iron Binding Motifs, Rachel Burke
The Synthesis And Biological Activity Of Iron Binding Motifs, Rachel Burke
Honors College Theses
Iron is an essential mineral that plays a key role in the oxygen transporting molecule hemoglobin. Iron also helps muscles store and use oxygen. Excess iron in the body can attract electrons, creating harmful oxygen radicals. Iron overload can be caused by several factors such as genetics, age, gender, and having received multiple red blood cell transfusions. Excess iron can lead to many diseases, such as arthritis, liver cirrhosis, heart disease, and several forms of cancer. Iron-chelating therapies work by binding free iron in the bloodstream and by reducing the amount of iron bound in transferrin, the iron transporting molecule. …
Total Synthesis Of Biologically Active Natural And Unnatural Products, Julia Heimberger
Total Synthesis Of Biologically Active Natural And Unnatural Products, Julia Heimberger
College of Graduate Studies: Theses & Dissertations
Herbarin A and B were isolated from the fungal strains of Cladosporium herbarum found in marine sponges Aplysina aerophoba and Callyspongia aerizusa. Total synthesis of Herbarin A and B was achieved by carrying out a multi-step synthesis approach, and the antioxidant properties were evaluated using FRAP assay. Toxicity of these compounds was determined using a zebrafish embryo model. Furthermore, synthesis of C-6 alkyl-azaarene derivatives of nucleosides by Csp3-H bond functionalization were investigated. Effective incorporation of 2-methylazaarene moiety at the C-6 position of the protected inosine nucleoside provided a new class of compounds with anticipated enhanced biological activity.