Physical Sciences and Mathematics Commons^™

Total Synthesis Of Cytotoxic Mansouramycins From Amino Acids, Beatriz Gamez

Theses and Dissertations

Natural products produced by plants, animals, and microorganisms are of significant importance in chemistry for being major sources of molecular scaffolds essential for new drug discovery. Mansouramycins are cytotoxic bioactive compounds containing isoquinoline skeletons with substituents on the quinone and pyridine rings that may be difficult to synthesize. Synthetic processes exist for compounds B and D, however, there exists an absence of simple synthetic approaches to all four alkaloids.

This project aims to provide a general total synthetic pathway to Mansouramycins A—D from amino acids for possible use in cancer treatment via these isoquinolinequinones. Preliminary experimentation suggests there may be …

Chemical Modification And In Silico Validation Of Medicinally Privileged Molecular Scaffolds As Kras And Sars-Cov-2 Protease Inhibitors, Precious M. Okwuchukwu

Theses and Dissertations

Coronavirus disease was declared a global pandemic by WHO in March 2020, cancer is the second leading cause of death by a disease. Several scientists around the world are working relentlessly to discover an effective remedy to eradicate these deadly diseases. A natural polyphenol (magnolol) has been isolated from a tree Magnolia grandiflora (family Magnoliaceae) found on UTRGV campuses. This research is focused on design of a series of chemically modified sulfonyl derivatives based on the isolated magnolol framework and other medicinally privileged molecular scaffolds framework that can effectively bind to the COVID-19 main protease, SARS- CoV-2 3CL protease …

Characterization Of Dna Interstrand Cross-Linking Agents By Liquid Chromatograhy-Mass Spectrometry, Anahit Marina Campbell

Theses and Dissertations

This study is to characterize novel reactive oxygen species (ROS)-activated nitrogen mustard analogues and UV-activated alkylating agents by Liquid Chromatography-Mass Spectrometry (LC-MS). First, we optimized the instrument conditions to successfully ionize a few novel binapthalene analogues and methoxybenzene analogues by MS. The highest signal intensity for compounds 3-10 was observed when atmospheric pressure chemical ionization (APCI) with an optimized corona needle position of 5mm or 10 mm was used, which led to successful analysis of compounds 3-10 by MS. Second, we determined pharmacokinetic properties of a drug compound (FAN-NM-CH3), including animal study, assay development, optimization of MS/MS instrumental parameter and …

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 …

Developing A New Water-Soluble Porphyrin As A Potential Photodynamic Cancer Therapy Agent, Catherine Shirley

Honors Theses

Photodynamic cancer therapy (PDT) is a type of treatment involving the use of light in conjunction with a photosensitive agent- a chemical or series of chemicals designed for activation when exposed to light. This research project investigated the synthesis and identification of the novel photosensitive agent, H2TPP-Pro-OH. To create the water-soluble porphyrin, (S)-(+)-prolinol was reacted with the tetra-carboxyl porphyrin, H2TPPC, to form the final H2TPP-Pro-OH product. This compound was then purified using syringe filtration and column chromatography, and subsequently characterized using infrared (IR), nuclear magnetic resonance (NMR), and Ultraviolet-visible (UV-vis) spectroscopies, as well as High Performance Liquid Chromatography (HPLC). Finally, …

Preparation And Cytotoxicity Of Novel Carbon Nano-Onion Materials, Cammie York

Honors Theses

The applications of carbon nanomaterials (CNM), including graphene and its derivatives such as carbon nanotubes (CNTs) in nanomedicine is well established. These nanomaterials have been widely used as theranostic delivery systems with the potential to deliver bioactive agents and simultaneously detect selectively diseased tissues. A rather underexplored CNM for biomedical imaging and theranostics delivery are carbon nano-onions (CNOs). CNOs are carbon-based nanomaterials that can potentially be used in cancer therapy when they are functionalized. Recent studies on cellular fate of different CNMs, including CNOs, have demonstrated that the surface composition is critical for the in vivo application of these CNM. …

Leveraging Antibodies For Positron Emission Tomography And Near-Infrared Fluorescence Imaging Of Cancer, Kimberly C. Fung

Dissertations, Theses, and Capstone Projects

The high specificity and affinity of antibodies make them attractive for developing drugs to diagnose and treat cancer. The overarching goal of this work is to explore the synthesis and use of antibody-based imaging agents in preclinical models of cancer. This work can be described as two-fold. In the first part, we investigated how the use of a glycans-specific bioconjugation strategy affects Fc gamma RI binding and why it results in improved in vivo performance of immunoconjugates. To do so, we used the clinically relevant positron emission tomography (PET) imaging agent, ⁸⁹Zr-DFO-pertuzumab, in mouse models of human breast cancer. …