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Medicinal-Pharmaceutical Chemistry Commons

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Full-Text Articles in Medicinal-Pharmaceutical Chemistry

Synthesis Of Multifunctional Polyacrylates And A Binding Group To Hemoglobin For The Treatment Of Traumatic Brain Injuries, Marina Michaud Jan 2017

Synthesis Of Multifunctional Polyacrylates And A Binding Group To Hemoglobin For The Treatment Of Traumatic Brain Injuries, Marina Michaud

University Honors Program 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 ...


Synthesis And Biological Activity Of Novel Tu100 Derivatives, Oladotun J. Alao Jan 2017

Synthesis And Biological Activity Of Novel Tu100 Derivatives, Oladotun J. Alao

Electronic Theses and 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.


Exploring The Relationship Of Mbd1 Protein Binding Cpg Sites Of Methylated Dna, Shelby L. Scherer Jan 2016

Exploring The Relationship Of Mbd1 Protein Binding Cpg Sites Of Methylated Dna, Shelby L. Scherer

University Honors Program 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 ...


The Study Of Nf-Κb Peptide Mimics And How Proteins Bind Dna, Allee M. Murray Jan 2016

The Study Of Nf-Κb Peptide Mimics And How Proteins Bind Dna, Allee M. Murray

University Honors Program 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 ...


Total Synthesis Of Biologically Active Natural And Unnatural Products, Julia Heimberger Jan 2015

Total Synthesis Of Biologically Active Natural And Unnatural Products, Julia Heimberger

Electronic Theses and 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.


The Synthesis And Biological Activity Of Iron Binding Motifs, Rachel Burke Jan 2014

The Synthesis And Biological Activity Of Iron Binding Motifs, Rachel Burke

University Honors Program 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 ...