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Full-Text Articles in Medicinal-Pharmaceutical Chemistry

Development Of Neurotensin-Based Radiopharmaceuticals For Neurotensin-Receptor-1-Positive Tumors Targeting, Yinnong Jia May 2017

Development Of Neurotensin-Based Radiopharmaceuticals For Neurotensin-Receptor-1-Positive Tumors Targeting, Yinnong Jia

Theses & Dissertations

The neurotensin receptor 1 (NTR1) is overexpressed in many cancers, due to its role as a growth pathway. These NTR1-positive cancers include pancreatic, colon, prostate and breast cancers. In the radiopharmaceutical field, the overexpression of NTR1 in cancer has prompted the development of NTR1-targeted diagnostics and therapeutics. The neurotensin (NT) peptide exhibits low nanomolar affinity for NTR1 and has been the paradigm for NTR1-targeted agents. Since the 1980’s, radiolabeled NT analogs have been developed and evaluated for targeting NTR1-positive cancers. Since native NT is rapidly degraded in vivo by a variety of peptidases, a tremendous amount of effort has ...


Synthesis Of A Novel Cox-2 Inhibitor Analog For Pet Scan Imaging, Rebecca Neighbor May 2016

Synthesis Of A Novel Cox-2 Inhibitor Analog For Pet Scan Imaging, Rebecca Neighbor

Chancellor’s Honors Program Projects

No abstract provided.


The Design And Synthesis Of Ghrelin Analogues As Non‐Invasive Ghs‐R1a Imaging Probes, Carlie L. Charlton Feb 2016

The Design And Synthesis Of Ghrelin Analogues As Non‐Invasive Ghs‐R1a Imaging Probes, Carlie L. Charlton

Electronic Thesis and Dissertation Repository

The field of molecular imaging is constantly growing and evolving in order to provide the best possible healthcare for patients in various stages of disease and therapy. Molecular imaging aims to locate specific markers of disease by selectively targeting the markers of interest with high selectivity and visualizing the accumulation using external detection. The growth hormone secretagogue receptor-1a (GHS-R1a) has been shown to be involved in various important biological functions such as energy homeostasis and cardiac contractility. GHS-R1a has shown involvement in proliferation, migration and cell invasion of specific cancer subtypes. Therefore, targeting GHS-R1a is an important marker of different ...


Investigation Of 89zr-Siderophores As Molecular Imaging Agents For Positron Emission Tomography Imaging Of Bacterial Infections, Nora C. M. Goscinski Dec 2015

Investigation Of 89zr-Siderophores As Molecular Imaging Agents For Positron Emission Tomography Imaging Of Bacterial Infections, Nora C. M. Goscinski

Arts & Sciences Electronic Theses and Dissertations

Siderophores are small molecules synthesized by bacteria to harvest Fe3+ from their environment. In infection scenarios, their production can increase infection virulence by increasing the ability of bacteria to obtain Fe3+ and therefore grow more rapidly. The selective uptake of siderophores in vivo in multi-bacteria environments indicates that this class of molecules has a potential use as selective imaging agents. In this work, DFO-NCS and a library of trihydroxamate siderophores were evaluated as vehicles to deliver 89Zr selectively to bacteria for Positron Emission Tomography (PET) imaging of bacterial infections.

Productive work with radiometals involves thorough knowledge of ...


Uses Of Diaryliodonium Salts And Methods For Their Synthesis, Jordan M. Veness Dec 2015

Uses Of Diaryliodonium Salts And Methods For Their Synthesis, Jordan M. Veness

Student Research Projects, Dissertations, and Theses - Chemistry Department

Diaryliodonium salts have been studied continuously since the first report of their synthesis in 1894. Diaryliodonium salts are I(III) derivatives that are air- and moisturestable. The reactivity of these compounds resembles the organometallic chemistry of heavy transition metal ions such as Pb(IV), Hg(II), Th(III), and Pd(II). A significant advantage of diaryliodonium salts is that they can carry undergo many of the aryl functionalization reactions of heavy metal organometallic complexes, yet they have little to no toxicity and they are relatively inexpensive to prepare. The DiMagno laboratory uses diaryliodonium salts as precursors in the final synthetic ...


Green Chemistry As A Tool For Understanding The Toxic Substances Control Act: A Lecture Module For Undergraduate Students, Molly R. Blessing May 2015

Green Chemistry As A Tool For Understanding The Toxic Substances Control Act: A Lecture Module For Undergraduate Students, Molly R. Blessing

Honors Scholar Theses

The Toxic Substances Control Act (TSCA) is the central form of chemical regulation existent in the United States today, yet scientists are often unaware or uncertain of its provisions. Violations of TSCA by unknowing chemists set industry and government unnecessarily at odds. A lecture on TSCA was developed for undergraduate students that uses the concept of green chemistry to promote interest and incentivize learning. Green chemistry methods are cleaner and less wasteful than traditional chemical ones, and many companies using them are at the forefront of technological innovation. The lecture explains both green chemistry and TSCA, includes company case studies ...


Development Of A Gallium-Containing One-Bead One-Compound Peptide Library For The Discovery Of New Molecular Imaging Probes, Fernanda C. Bononi Aug 2014

Development Of A Gallium-Containing One-Bead One-Compound Peptide Library For The Discovery Of New Molecular Imaging Probes, Fernanda C. Bononi

Electronic Thesis and Dissertation Repository

An eight amino acid one-bead one-compound (OBOC) peptide library, containing a gallium-DOTA complex, was developed in an attempt to overcome common issues associated with the later addition of radionuclides to peptide chains of imaging probes. The further addition of a radionuclide often changes the binding properties of a peptide, as it adds bulk, and possibly charges. MALDI (matrix-assisted laser desorption ionization) tandem mass spectrometry was determined to be the method of choice in order to deconvolute gallium-containing peptide sequences. The library obtained was screened against the breast cancer cell lines MDA-MB-231 and MCF-7. Positive beads were isolated and sequences were ...


Syntheses Of Precursors To Fluorine-18 Labeled Pet Imaging Agents, Lindsay B. Boling May 2014

Syntheses Of Precursors To Fluorine-18 Labeled Pet Imaging Agents, Lindsay B. Boling

Chancellor’s Honors Program Projects

No abstract provided.


Radiopharmaceuticals: The Application Of Technetium-99m And Rhenium Complexes, Angela Kristin Binion May 2014

Radiopharmaceuticals: The Application Of Technetium-99m And Rhenium Complexes, Angela Kristin Binion

Syracuse University Honors Program Capstone Projects

Nuclear imaging used in diagnostic medicine requires the use of radiopharmaceuticals to make biological areas visible under a gamma camera. Although much success has been found in the use of technetium based imaging agents, their corresponding rhenium complexes can provide insight into the chemical properties of these radiopharmaceuticals without the potentially damaging effects of radiation. Technetium and rhenium complexes utilize a bifunctional chelator to act as a linker between biological vectors and the metal, improving the coordination between the two. Ligands containing thiazole rings have been successfully coordinated to technetium or rhenium tricarbonyl complexes, although it is uncertain whether coordination ...


Peptidomimetic Ghs-R1a Agonists As Pet Imaging Agents For Prostate Cancer, Milan M. Fowkes Apr 2014

Peptidomimetic Ghs-R1a Agonists As Pet Imaging Agents For Prostate Cancer, Milan M. Fowkes

Electronic Thesis and Dissertation Repository

Contemporary diagnostic techniques for prostate cancer (PCa) have a limited ability to distinguish between benign and malignant disease. The ghrelin receptor has a differential expression in normal, benign and cancerous prostatic tissue. Targeting this receptor with 18F-radiolabelled peptidomimetics would enable differentiation between these disease states via PET imaging. A series of 19F-peptidomimetics were synthesized and characterized by HRMS, HPLC and 1 H-NMR spectroscopy in order to test locations for 18F radioisotope insertion. Competitive receptor binding assays using HEK293/GHS-R1a cells were used to evaluate compound binding affinities. This led to the identification of two lead compounds: [1-Nal4,Lys5(4-FB)]G-7039 ...


A. Catalysis Of Co-Prox By Water-Soluble Rhodium Fluorinated Porphyrins B. Studies Toward Fluorination Of Electron Rich Aromatics By Nucleophilic Fluoride, Shri Harsha Uppaluri Jul 2013

A. Catalysis Of Co-Prox By Water-Soluble Rhodium Fluorinated Porphyrins B. Studies Toward Fluorination Of Electron Rich Aromatics By Nucleophilic Fluoride, Shri Harsha Uppaluri

Student Research Projects, Dissertations, and Theses - Chemistry Department

The rhodium(III) derivative of a water soluble, heavily fluorinated porphyrin is shown to catalyze the low temperature, low pressure selective oxidation of carbon monoxide in hydrogen gas streams for use in fuel cell applications. The catalytic activity is a direct result of the removal of electron density from the metal center. Selectivity for CO oxidation is a direct consequence of fluorination of the porphyrin periphery, since these substituents enhance the rate of the reaction and prevent the formation of Rh(II)-Rh(II) dimmers. Significantly, the dramatic increase in rhodium hydride acidity caused by fluorination precludes hydrogen activation and ...


Electrochemistry Of Technetium Analogues Rhenium And Molybdenum In Room Temperature Ionic Liquid, Pauline Nancy Serrano Jun 2011

Electrochemistry Of Technetium Analogues Rhenium And Molybdenum In Room Temperature Ionic Liquid, Pauline Nancy Serrano

UNLV Theses, Dissertations, Professional Papers, and Capstones

Rhenium was used as an analog for Technetium to study the electrochemical redox properties because the two elements share the same stable oxidation states in aqueous solutions. However, Tc-99 is radioactive and is not readily available for experimentation purposes. Molybdenum is also of interest because when Mo-99 is irradiated, the decay products are Tc-99m and Tc-99. Approximately 30% Tc-99m is eluted from the Mo columns for radiopharmaceutical use with the remaining Mo-99 source decaying to Tc-99 which is discarded as radioactive hospital waste. Currently there are no viable procedures for the reclamation of the radioactive Tc-99 from either fission streams ...