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Synthesis And Characterization Of Gd-Doped Inp/Zns Quantum Dots For Use In Multimodal Imaging Probes, Molly Erin Duszynski Aug 2019

Synthesis And Characterization Of Gd-Doped Inp/Zns Quantum Dots For Use In Multimodal Imaging Probes, Molly Erin Duszynski

Graduate Theses/Dissertations

Quantum dots (QDs), which are intensely fluorescent nanocrystals ranging 2-10 nanometers in diameter, have shown promise in fluorescence imaging. However, in vivo applications of QDs are limited due to the opaque surrounding of tissue and bones. In this study, InP/ZnS QDs were doped with a paramagnetic atom in an attempt to render them MRI-active. We have further bioconjugated these nanoprobes to develop highly specific MRI-active probes that can be used for detection of neurodegenerative diseases. These bioconjugated nanoprobes detect a mutated form of alpha-synuclein that forms oligomers that are a hallmark of Parkinson’s disease andother alpha-synucleinopathies. Here, we have optimized …


Acid-Mediated N-Iodosuccinimide-Based Thioglycoside Activation For The Automated Solution-Phase Synthesis Of Α-1,2-Linked-Rhamnopyranosides, Victoria R. Kohout, Alyssa L. Pirinelli, Nicola L.B. Pohl Jul 2019

Acid-Mediated N-Iodosuccinimide-Based Thioglycoside Activation For The Automated Solution-Phase Synthesis Of Α-1,2-Linked-Rhamnopyranosides, Victoria R. Kohout, Alyssa L. Pirinelli, Nicola L.B. Pohl

Chemistry Publications

Carbohydrate structures are often complex. Unfortunately, synthesis of the range of sugar combinations precludes the use of a single coupling protocol or set of reagents. Adapting known, reliable bench-chemistry reactions to work via automation will help forward the goal of synthesizing a broad range of glycans. Herein, the preparation of di- and tri-saccharides of alpha 1→2 rhamnan fragments is demonstrated using thioglycoside donors with the development for a solution-phase-based automation platform of commonly used activation conditions using N-iodosuccinimide (NIS) with trimethylsilyl triflate. Byproducts of the glycosylation reaction are shown to be compatible with hydrazine-based deprotection conditions, lending broader functionality …


The Alpha-Activator Complex, Cellular Maturation, And Catalytic Mechanism Of Iron-Type Nitrile Hydratase, Wasantha Lankathilaka Karunagala Pathiranage Jul 2019

The Alpha-Activator Complex, Cellular Maturation, And Catalytic Mechanism Of Iron-Type Nitrile Hydratase, Wasantha Lankathilaka Karunagala Pathiranage

Dissertations (1934 -)

In industry, chemicals are typically synthesized through catalytically accelerated chemical processes. The use of biocatalysts is an increasingly important trend in achieving environmentally friendly chemical production processes. Nitrile Hydratases (NHases) are well-known biocatalysts that are used by several manufacturers such as Mitsubishi Rayon Corporation and Lonza for the conversion of acrylonitrile to acrylamide and 3-cyanopyridine to nicotinamide, respectively. Amides, in general, are used in polymer preparation, adhesive manufacturing, and the paper industry. Refrigeration is needed in the enzymatic hydration process on the industrial scale to maintain a low reaction temperature to stabilize the NHase enzyme. The use of whole cells …


Synthesis And Evaluation Of 1,2,4-Oxadiazolidinones: The Search For A Potential Non-Β-Lactam Β-Lactamase Inhibitors., Chimdi Eke Kalu May 2019

Synthesis And Evaluation Of 1,2,4-Oxadiazolidinones: The Search For A Potential Non-Β-Lactam Β-Lactamase Inhibitors., Chimdi Eke Kalu

Electronic Theses and Dissertations

β-lactam antibiotics have been the most widely used drug of choice to combat infectious disease caused by bacteria. Unfortunately, their effectiveness is drastically threatened by bacterial β-lactamases. β-lactamases is responsible for the resistance to most antibiotic drugs. For decades, β-lactam β-lactamases inhibitors have been used to reduce bacterial resistance; however, in this study 1,2,4-oxadiazolidinone derivatives as a non-β-lactam β-lactamases inhibitor against TEM-1 and P99 β-lactamases. The significance of oxadiazolidinone is the prominent five-membered ring scaffold in its structure, which is configurationally stable and present in other biologically active compounds such as linezolid and avibactam. Oxadiazolidinones were synthesized by treating nitrones …


Design And Synthesis Of 5-Oxo-Ete Receptor Antagonists; And Synthesis Of Neuroprostanes As A Biomarker For The Diagnosis Of Alzheimer’S Disease, Rui Wang May 2019

Design And Synthesis Of 5-Oxo-Ete Receptor Antagonists; And Synthesis Of Neuroprostanes As A Biomarker For The Diagnosis Of Alzheimer’S Disease, Rui Wang

Theses and Dissertations

1) 5-Oxo-ETE (7, Scheme 1) is the most potent eosinophil chemoattractant among all lipid mediators and it can also stimulate a late-phase asthma attack. It is formed by the biotransformation of arachidonic acid (AA, 1, Figure 1). 5-Oxo-ETE (7) elicits eosinophil migration both in vitro and in vivo when injected intradermally in humans, acting via the highly selective OXE receptor (OXE-R). Our group postulated that a selective OXE-R antagonist might be a useful therapeutic agent in late phase asthma. As a result, the first and only series of OXE receptor antagonists which are structural mimics of 5-oxo-ETE (7) have been …


Synthetic Methods And Biological Applications Of Nitrogen Heterocycles To Compounds Of Biological Interest., Jarrid Ronnebaum May 2019

Synthetic Methods And Biological Applications Of Nitrogen Heterocycles To Compounds Of Biological Interest., Jarrid Ronnebaum

Electronic Theses and Dissertations

Thalidomide analogues were synthesized utilizing optimized click conditions from 3-azidoglutarimide and an array of arylacetylenes or N-ethynyl/N-propargyl phthalimide derivatives. The intermediate, 3-azidoglutarimde, was pivotal and yielded a new and scalable synthesis. The reaction conditions utilized a copper sulfate/sodium ascorbate system in aqueous tetrahydrofuran to propagate the dipolar cycloaddition reactions between the azidoglutarimide and the alkynyl coupling partners. The first explored substrates were substituted arylalkynes to optimize the click reaction. Arylalkynes selected were to exhibit similar electron deficient rings to mimic phthalimide. Along with the synthesis of click thalidomide analogues, click analogue of the antiangiogenic and more potent …


Application Of The Picoloyl Group In Carbohydrate Chemistry, Michael Mannino Apr 2019

Application Of The Picoloyl Group In Carbohydrate Chemistry, Michael Mannino

Dissertations

Stereocontrol of glycosylation reactions is a constant struggle in the field of synthetic carbohydrate chemistry. The application of the picoloyl (Pico) substituent can offer numerous stereocontrolling avenues. The most popular application is the Hydrogen-bond-mediated Aglycone Delivery (HAD) method that provides excellent selectivity in the glycosylation of a variety of sugar substrates. The HAD method relies on the formation of an intermolecular hydrogen bond between the nitrogen atom of the Pico substituent on the glycosyl donor with the hydroxyl group of the glycosyl acceptor. This interaction provides a facial preference for the nucleophilic attack and hence provides powerful stereocontrol for the …


The Potential Of Marine Microbes, Flora And Fauna In Drug Discovery, Santana Alexa Lavonia Thomas Apr 2019

The Potential Of Marine Microbes, Flora And Fauna In Drug Discovery, Santana Alexa Lavonia Thomas

USF Tampa Graduate Theses and Dissertations

Natural products are chemical compounds synthesized by a living organism. These compounds have been utilized by humans from ancient times to the present for their pharmacological and biological activities. Terrestrial organisms are considered a lucrative source of bioactive compounds and chemical diversity. Within the past 60 years, the marine environment has presented its potential as a validated source for structural diversity and biologically active compounds. Technology has given access from shallow waters down to the abyssal plane for exploration and investigation of the inhabitants. Marine organisms have displayed their benefits in the pharmaceutical industry with the approval of several marine-derived …


Structural Studies Of Dna Repeats Implicated In Cancer, Deondre Jordan , '19 Apr 2019

Structural Studies Of Dna Repeats Implicated In Cancer, Deondre Jordan , '19

Senior Theses, Projects, and Awards

DNA replication is an essential process for the survival of all organisms. Errors can occur during the process that leads to replication stress, which can promote genomic instability, a hallmark of cancer. The Brown lab conducted a genome wide study to identify sites and sequences linked to replication stress. Tandem DNA repeats comprised the sequences identified in this study. One particular DNA repeat (CAGAGG)ₙ stood out due to being highly associated with replication stress. Repeats such as (CAGAGG)ₙ are believed to fold into fold into intramolecular structures that physically block DNA polymerase during replication. Understanding the structures of these problematic …


Synthesis, Characterization, And Nonlinear Optical Properties Of Some New Series Of S-(5-Aryl-1,3,4-Oxadiazol-2-Yl) 2-Chloroethanethioate Derivatives, Zahra Dono Ghezelbash, Hamideh Motiei, Miri Mahmoody, Karim Akbari Delmaghani Jan 2019

Synthesis, Characterization, And Nonlinear Optical Properties Of Some New Series Of S-(5-Aryl-1,3,4-Oxadiazol-2-Yl) 2-Chloroethanethioate Derivatives, Zahra Dono Ghezelbash, Hamideh Motiei, Miri Mahmoody, Karim Akbari Delmaghani

Turkish Journal of Chemistry

In the present investigation, some novel S-(5-aryl-1,3,4-oxadiazol-2-yl)2-chloroethanethioate (3a-3e) derivatives were synthesized and their impact on optical properties was studied. They have also been characterized by elemental analysis and various spectroscopic methods including FTIR, $^{1}$H NMR, $^{13}$C NMR, and UV-Vis techniques. The nonlinear refractive indexes of 3a-3e were also measured in dichloromethane via Z-scan method using a continuous wave diode-pumped laser at 532 nm wavelength. The nonlinear refractive coefficient of compounds was obtained from ${10}^{11}\, \, {m}^{{2}}{/W}$ order. Regarding the appropriate nonlinearity of these compounds, they could be considered good candidates for biooptical and photonic applications. All the synthesized compounds (3a-3e) …


Synthesis Of Smz Derivatives And Investigation Of Effects On Germination, Root, And Plant Growth Of \Textit{Arabidopsis Thaliana} L., Tuğba Güngör, Ferah Cömert Önder, Fati̇h Sezer, Aslihan Özbi̇len, Kemal Meli̇h Taşkin, Mehmet Ay Jan 2019

Synthesis Of Smz Derivatives And Investigation Of Effects On Germination, Root, And Plant Growth Of \Textit{Arabidopsis Thaliana} L., Tuğba Güngör, Ferah Cömert Önder, Fati̇h Sezer, Aslihan Özbi̇len, Kemal Meli̇h Taşkin, Mehmet Ay

Turkish Journal of Chemistry

A series of sulfonamide derivatives were synthesized by reactions with various functional groups containing benzenesulfonyl chlorides and aniline derivatives under different substitution reaction conditions. The structures of SMZ derivatives were confirmed with melting point, FT-IR, $^{1}$H NMR, $^{13}$C NMR, and LC-MS/MS techniques. In order to investigate the cytotoxic effects of these derivatives, we used a model plant species. The synthesized compounds (S1-S5) and sulfamethazine (SMZ) as a positive control were applied to Arabidopsis thaliana seeds. Our results indicated that S3 and S4 induced shorter roots and lower wet weight in plants. Plants treated with S2 and S5 showed no growth …


Design, Synthesis, Biological Evaluation And Molecular Docking Of Novel Molecules To Parp-1 Enzyme, Fati̇h Tok, Bedi̇a Kaymakçioğlu, Recep İlhan, Si̇nem Yilmaz, Petek Ballar Kirmizibayrak, Tuğba Taşkin Tok Jan 2019

Design, Synthesis, Biological Evaluation And Molecular Docking Of Novel Molecules To Parp-1 Enzyme, Fati̇h Tok, Bedi̇a Kaymakçioğlu, Recep İlhan, Si̇nem Yilmaz, Petek Ballar Kirmizibayrak, Tuğba Taşkin Tok

Turkish Journal of Chemistry

Poly (ADP-ribose) polymerase (PARP) enzyme catalyzes the transfer of ADP-ribose into target proteins. Therefore, PARP is responsible for DNA repair, cell proliferation, and cell death. In this study, potential PARP enzyme inhibitors were designed and synthesized. The synthesized compounds were elucidated by Fourier-transform infrared spectroscopy, $^{1}$H NMR, $^{13}$C NMR, heteronuclear single-quantum correlation, and mass spectrometry, and their purity was checked via thin-layer chromatography, high-performance liquid chromatography, and elemental analysis. A total of 63 newly synthesized compounds were screened in terms of PARP inhibition by cellular PARylation assay in the HeLa cell line. It was found that 19 compounds significantly inhibited …


In Silico And In Vitro Evaluation Of The Biological Activity Of Some Organic Sulfur-Containing Compounds, Victoria Osipova, Maria Polovinkina, Anastasia Osipova, Yulia Gracheva, Andrey Okhlobystin Jan 2019

In Silico And In Vitro Evaluation Of The Biological Activity Of Some Organic Sulfur-Containing Compounds, Victoria Osipova, Maria Polovinkina, Anastasia Osipova, Yulia Gracheva, Andrey Okhlobystin

Turkish Journal of Chemistry

It was predicted, using the Prediction of Activity Spectra for Substances online software, that organic sulfur-containing compounds 2,6-di-tert-butyl-4-mercaptophenol (1), 2,6-di-tert-butyl-4-(3-mercaptopropyl)phenol (2), bis-3-[3,5-di-tert-butyl-4-hydroxyphenyl)propyl] sulfide (3), bis(3,5-di-tert- butyl-4-hydroxyphenyl) disulfide (4), diphenyl disulfide (5), dibenzyl disulfide (6), dibutyl disulfide (7), di-tert-butyl disulfide (8), diallyl disulfide (9), and methyl propyl trisulfide (10) could possess antioxidant activity and act as active scavengers of oxygen metabolites. The antiradical activity of these species was analyzed and it was shown that they were able to react with electrochemically generated the superoxide anion radical. The rate constants for reactions of 1-10 with the superoxide anion radical were calculated. The …


N-Methyl Mesoporphyrin Ix As A Highly Selective Light-Up Probe For G-Quadruplex Dna, Ariana Yett , '21, Linda Yingqi Lin , '20, Dana Beseiso , '21, Joanne Miao , '22, Liliya A. Yatsunyk Jan 2019

N-Methyl Mesoporphyrin Ix As A Highly Selective Light-Up Probe For G-Quadruplex Dna, Ariana Yett , '21, Linda Yingqi Lin , '20, Dana Beseiso , '21, Joanne Miao , '22, Liliya A. Yatsunyk

Chemistry & Biochemistry Faculty Works

N-methyl mesoporphyrin IX (NMM) is a water-soluble, non-symmetric porphyrin with excellent optical properties and unparalleled selectivity for G-quadruplex (GQ) DNA. G-quadruplexes are non-canonical DNA structures formed by guanine-rich sequences. They are implicated in genomic stability, longevity, and cancer. The ability of NMM to selectively recognize GQ structures makes it a valuable scaffold for designing novel GQ binders. In this review, we survey the literature describing the GQ-binding properties of NMM as well as its wide utility in chemistry and biology. We start with the discovery of the GQ-binding properties of NMM and the development of NMM-binding aptamers. We then discuss …


In-Silico Design And Synthesis Of Selective Estrogen Receptor Modulators Targeting Ovarian Cancer, John Apraku Jan 2019

In-Silico Design And Synthesis Of Selective Estrogen Receptor Modulators Targeting Ovarian Cancer, John Apraku

Electronic Theses and Dissertations

The established records of the safety of Ormeloxifene along with its favorable bioavailability and ability to inhibit rapid cell proliferation in the endometrium during embryonic implantation has made it one of the best drug candidates for controlling undesirable rapid cell growth such as endometriosis and cancerous tumor conditions. Recent studies have confirmed the effectiveness of Ormeloxifene to suppress and inhibit epithelial-mesenchymal transition process as evidenced by repression of N-cadherin, slug, snail, vimentin, MMPs, β-catenin/TCF-4 transcriptional activity and induce the expression of pGSK3b. Recently conducted studies have revealed the dynamic binding of ormeloxifene with β-catenin, GSK3b, CDK4, and other downstream EGFR. …


A Study To Regioselectively Access Fluorinated Triazoles And Isoxazoles, Sweta Adhikari Jan 2019

A Study To Regioselectively Access Fluorinated Triazoles And Isoxazoles, Sweta Adhikari

Electronic Theses and Dissertations

The objective of the thesis is to develop regioselective methods for mono-fluorination of disubstituted triazoles, both 1,4- and 1,5-regioisomer, and isoxazoles. These strategies focus on one-pot direct access to final mono-fluorinated triazoles and isoxazoles. Eventually, these fluorinated substrates will be screened against various biological targets. Similarly, the optimization study of a regioselective method to generate 5-fluoro-1,4-disubstituted triazole was conducted. This reaction also utilized 1,3-dipolar cycloaddition to synthesize fluorinated triazole. However, difluoroalkene was used as a synthetic equivalent of fluoroalkyne for this method. This resulted into the inversion of polarity affording a different regioisomer. Here, fluoronitroalkene was identified as a synthetic …


Oleic Acid Vesicles: Formation, Mechanisms Of Reactivity, And Uses In Determination Of Terpene Activity, Laura A. Walther Jan 2019

Oleic Acid Vesicles: Formation, Mechanisms Of Reactivity, And Uses In Determination Of Terpene Activity, Laura A. Walther

Theses and Dissertations--Chemistry

This dissertation will focus on the volatile compounds released upon the burning of incense which are numerous and varied. The first part of this dissertation is the gas chromatography-mass spectral (GC-MS) analysis of burning incense collected via solid phase microextraction (SPME) with the aim of developing a library of compounds found in incense as used in the Orthodox church.

The second part of this dissertation has the aim of developing a method for forming oleic acid bilayer vesicle membranes and a fluorescence spectroscopy method by which the reactivities of these vesicles can be analyzed. These reactivities include permeability, fluidity, aggregation, …


Synthesis And Development Of Nanocomposites Of Magnetic Nanoparticles-Silica-Mannan As Vaccine Adjuvants, Kamonlatth Rodponthukwaji Jan 2019

Synthesis And Development Of Nanocomposites Of Magnetic Nanoparticles-Silica-Mannan As Vaccine Adjuvants, Kamonlatth Rodponthukwaji

Chulalongkorn University Theses and Dissertations (Chula ETD)

Over the past years, vaccination has been considered as an effective treatment against a wide range of pathogens and diseases. Despite a promising outcome, the lack of strong immune response of some types of vaccines is still challenging. Therefore, targeting and activating dendritic cells (DCs) using nanomaterial-based vaccine adjuvant is of our interest. Herein, superparamagnetic iron oxide nanoparticles (SPIONs) have been exploited as directing agents to the targeted dendritic cells (DCs). In addition, mannan extracted from Saccharomyces cerevisiae was used as targeting molecules for targeting DCs. Nanocomposites of silica-magnetic nanoparticles-mannan (S-SPION-MN) were successfully fabricated. The synthesized particles were morphologically and …


Chemical Synthesis Of Galacto-Oligosaccharides And Evaluation Of Their Prebiotic Properties, Pranpariya Ponpakdee Jan 2019

Chemical Synthesis Of Galacto-Oligosaccharides And Evaluation Of Their Prebiotic Properties, Pranpariya Ponpakdee

Chulalongkorn University Theses and Dissertations (Chula ETD)

Galacto-oligosaccharides (GOS) are composed of galactose and glucose between 2–8 units or disaccharide comprising 2 units of galactose linked by glycosidic bonds. GOS exhibits prebiotic activity and widely used in infant formula. Commercial GOS was achieved as mixture by enzymatic synthesis of lactose with β-galactosidase. Due to the nature of the enzymatic derived-GOS, the structure-activity relationship of GOS and prebiotic activity is mainly ambiguous. In this work, we presented the development towards a production of GOS by chemical synthesis starting from lactose. First, lactose was isolated from liquid whey with 3.90% w/v recovery. Lactose was then hydrolyzed to produce galactose …


Green Synthesis/Biosynthesis Of Silver Nanoparticles By Using Orange Peel Extract, Leela Joshi Dec 2018

Green Synthesis/Biosynthesis Of Silver Nanoparticles By Using Orange Peel Extract, Leela Joshi

Theses and Dissertations

Joshi, Leela, Green Synthesis/Biosynthesis of Silver Nanoparticles by Using Orange Peel Extract. Master of Science (MS), December, 2018, 40 pages, 23 figures, references, 36 titles. In this work, we report synthesis of silver nanoparticles (AgNPs) with an average size of ~6 nm. The aqueous solution of Ag+ ions is reduced using an aqueous extract from orange peel (Citrus Sinensis) at varying pHs. Reduction of Ag+ ions in solution was monitored using UV-visible absorption spectroscopy, and the corresponding surface plasmon resonance of AgNPs at 435 nm. The solution changed color from yellow to reddish-brown upon bioreduction of silver nitrate in orange …


Carbon Monoxide On Demand: Light-Induced Co Release Of Flavonols, Stacey N. Anderson Dec 2018

Carbon Monoxide On Demand: Light-Induced Co Release Of Flavonols, Stacey N. Anderson

All Graduate Theses and Dissertations, Spring 1920 to Summer 2023

Carbon monoxide (CO) is an extremely useful molecule with applications in industrial manufacturing, synthetic procedures as a C1 building block, and as a potential pharmaceutical to produce anti-inflammatory effects and vasodilation. However, the toxicity associated with CO has prevented its full utilization. In order to safely handle CO, compounds and molecules have been developed that act as storage materials for the gas. Ideal storage platforms only release CO upon stimulation via a trigger. Light activation is the most desirable trigger as it can be regulated in terms of the intensity and the wavelength of light used. The majority of light-induced …


Development Of Functional Chemical Probes For The Study Of Viscosity, Fe(Ii), And Ferroptosis And Photo-Triggered Drug Delivery, Yongyi Wei Nov 2018

Development Of Functional Chemical Probes For The Study Of Viscosity, Fe(Ii), And Ferroptosis And Photo-Triggered Drug Delivery, Yongyi Wei

Chemistry and Chemical Biology ETDs

Small molecule probes are useful tools for the study of biology. In particular, the dye derived fluorescence probes enable to spatiotemporally monitor the events of analytes of interest. The noninvasive feature is particularly attractive for the biological studies in live cells. The challenge is to develop chemical probes capable of detection of the analyte of interest with high specificity.

Toward this end, my Ph. D. study centers on the development of novel chemical probes for the study and understanding of the alternation of important cellar contents and substances and their functions and relationship between normal and disease states. In the …


Intranasal Rapamycin Ameliorates Alzheimer-Like Cognitive Decline In A Mouse Model Of Down Syndrome, Antonella Tramutola, Chiara Lanzillotta, Eugenio Barone, Andrea Arena, Ilaria Zuliani, Luciana Mosca, Carla Blarzino, D. Allan Butterfield, Marzia Perluigi, Fabio Di Domenico Nov 2018

Intranasal Rapamycin Ameliorates Alzheimer-Like Cognitive Decline In A Mouse Model Of Down Syndrome, Antonella Tramutola, Chiara Lanzillotta, Eugenio Barone, Andrea Arena, Ilaria Zuliani, Luciana Mosca, Carla Blarzino, D. Allan Butterfield, Marzia Perluigi, Fabio Di Domenico

Chemistry Faculty Publications

Background: Down syndrome (DS) individuals, by the age of 40s, are at increased risk to develop Alzheimer-like dementia, with deposition in brain of senile plaques and neurofibrillary tangles. Our laboratory recently demonstrated the disturbance of PI3K/AKT/mTOR axis in DS brain, prior and after the development of Alzheimer Disease (AD). The aberrant modulation of the mTOR signalling in DS and AD age-related cognitive decline affects crucial neuronal pathways, including insulin signaling and autophagy, involved in pathology onset and progression. Within this context, the therapeutic use of mTOR-inhibitors may prevent/attenuate the neurodegenerative phenomena. By our work we aimed to rescue mTOR signalling …


Interactions Between Spermine-Derivatized Tentacle Porphyrins And The Human Telomeric Dna G-Quadruplex, Navin C. Sabharwal , '14, Jessica Chen , '17, Joo Hyun Lee , '17, C. M. A. Gangemi, A. D'Urso, Liliya A. Yatsunyk Nov 2018

Interactions Between Spermine-Derivatized Tentacle Porphyrins And The Human Telomeric Dna G-Quadruplex, Navin C. Sabharwal , '14, Jessica Chen , '17, Joo Hyun Lee , '17, C. M. A. Gangemi, A. D'Urso, Liliya A. Yatsunyk

Chemistry & Biochemistry Faculty Works

G-rich DNA sequences have the potential to fold into non-canonical G-Quadruplex (GQ) structures implicated in aging and human diseases, notably cancers. Because stabilization of GQs at telomeres and oncogene promoters may prevent cancer, there is an interest in developing small molecules that selectively target GQs. Herein, we investigate the interactions of meso-tetrakis-(4-carboxysperminephenyl)porphyrin (TCPPSpm4) and its Zn(II) derivative (ZnTCPPSpm4) with human telomeric DNA (Tel22) via UV-Vis, circular dichroism (CD), and fluorescence spectroscopies, resonance light scattering (RLS), and fluorescence resonance energy transfer (FRET) assays. UV-Vis titrations reveal binding constants of 4.7 × 10⁶ and 1.4 × 10⁷ M⁻¹ and binding stoichiometry of …


Synthesis And Biological Evaluation Of Phaeosphaeride A Derivatives As Antitumor Agents, Victoria Abzianidze, Petr Beltyukov, Sofya Zakharenkova, Natalia Moiseeva, Jennifer Mejia, Alvin Holder, Yuri Trishin, Alexander Berestetskiy, Victor Kuznetsov Nov 2018

Synthesis And Biological Evaluation Of Phaeosphaeride A Derivatives As Antitumor Agents, Victoria Abzianidze, Petr Beltyukov, Sofya Zakharenkova, Natalia Moiseeva, Jennifer Mejia, Alvin Holder, Yuri Trishin, Alexander Berestetskiy, Victor Kuznetsov

Chemistry & Biochemistry Faculty Publications

New derivatives of phaeosphaeride A (PPA) were synthesized and characterized. Anti-tumor activity studies were carried out on the HCT-116, PC3, MCF-7, A549, К562, NCI-Н929, Jurkat, THP-1, RPMI8228 tumor cell lines, and on the HEF cell line. All of the compounds synthesized were found to have better efficacy than PPA towards the tumor cell lines mentioned. Compound 6 was potent against six cancer cell lines, HCT-116, PC-3, K562, NCI-H929, Jurkat, and RPMI8226, showing a 47, 13.5, 16, 4, 1.5, and 7-fold increase in anticancer activity comparative to those of etoposide, respectively. Compound 1 possessed selectivity toward the NCI-H929 cell line (IC …


Synthesis And Evaluation Of Densely-Functionalized Troponoids, Danielle R. Hirsch Sep 2018

Synthesis And Evaluation Of Densely-Functionalized Troponoids, Danielle R. Hirsch

Dissertations, Theses, and Capstone Projects

Herein, we document our efforts to expand the scope of troponoid synthetic methodology towards densely-substituted scaffolds. This body of work has focused primarily on an oxidopyrylium cycloaddition/ring-opening strategy for the synthesis and biochemical evaluation of troponoids for assistance in a variety of medicinal chemistry studies. In Chapter 1, we outline the use of this synthetic strategy in the profiling of a library of synthetic αHTs against an aminoglycoside antibiotic resistance enzyme known as aminoglycoside-2’’-O-nucleotidyltransferase [ANT(2’’)-Ia]. Enzymatic mechanistic insights have been gleaned from an assessment of troponoid/antibiotic synergistic potential. In particular, two synthetic constructs were identified as promising antibiotic adjuvant candidates, …


Tof-Sims Analysis Of Plant Seed Interactions With Plant Growth-Promoting Bacteria, Tammy Pheuphong, Rachel Komorek, Xiao-Ying Yu Aug 2018

Tof-Sims Analysis Of Plant Seed Interactions With Plant Growth-Promoting Bacteria, Tammy Pheuphong, Rachel Komorek, Xiao-Ying Yu

STAR Program Research Presentations

The use of time-of-flight secondary ion mass spectrometry (ToF-SIMS) in plant biology is a relatively unexplored and quickly developing field. The majority of research in plant SIMS involves the application of ToF-SIMS to study dried wood tissues, and only a handful of studies apply SIMS on plant stems, roots, and/or seeds. Our project provides a brief description and review of previous work using SIMS on plant stems, roots, and/or seeds, along with an emphasis on the sample preparation in each study. Additionally, the use of Brachypodium distachyon (Brachypodium) as a model system for research on grasses has also become more …


Photochemical Expulsion Of Leaving Groups From A Naphthothiophene-2-Carboxamide Linked To A Chromophore, Lingzi Li Jul 2018

Photochemical Expulsion Of Leaving Groups From A Naphthothiophene-2-Carboxamide Linked To A Chromophore, Lingzi Li

Dissertations (1934 -)

Two bichromophoric systems were synthesized which have thioxanthone as the chromophore that absorbs the incident light and a naphthothiophene-2-carboxanilide, which serves as a triplet excited state energy acceptor. Upon excitation the triplet excited state of the thioxanthone is populated via intersystem crossing, which is efficient with isc = 0.68. Based on the relative energies of the triplet excited states of thioxanthone (ET = 65 kcal mol-1) and naphthothiophene (ET = 51 kcal mol-1), the subsequent triplet excited state energy transfer to generate the triplet excited state of the naphthothiophene-2-carboxamide should be a very rapid process that is 14 kcal mol1 …


Chemical Investigation Of Bioactive Marine Extracts, Selam Hagos Jun 2018

Chemical Investigation Of Bioactive Marine Extracts, Selam Hagos

USF Tampa Graduate Theses and Dissertations

Natural products have been a fundamental source of medicinal scaffolds for decades; with sixty percent of marketed drugs. Many synthetic chemists are focused on synthesizing potent and nontoxic compounds for pharmaceutical targets, however, nature is still proving to be a source of new bioactive compounds. Produced by the host organism for defense, reproduction and communication, secondary metabolites also demonstrate promising bioactivity against human pathogens. Hence, natural product chemists continue their quest for new leads.

As a continuation of these efforts, this thesis attempts to explore fungi and sponges for new chemistry, and ultimately, new drug candidates. Antarctica is largely untapped; …


Visualization And Quantification Of Cancer-Associated Enzymes With Fluorescent Small-Molecule Substrate Probes, Zhenhua Shen Jun 2018

Visualization And Quantification Of Cancer-Associated Enzymes With Fluorescent Small-Molecule Substrate Probes, Zhenhua Shen

LSU Doctoral Dissertations

Fluorescence imaging can be used both as a tool to diagnose diseases and guide treatment in clinical settings, and as a technique to monitor dynamic events or biological species in basic research. Therefore, there is a great need for the development of a multitude of fluorescent probes that can be incorporated with fluorescence imaging techniques to track and report endogenous enzymes with high specificity and selectivity. In contrast to always-on and targeted always-on fluorescent probes that continually emit light, activity-based substrate probes either emit low numbers of photons or are completely quenched. They can be converted to highly fluorescent reporters …