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Medicinal-Pharmaceutical Chemistry Commons

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2011

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Articles 1 - 9 of 9

Full-Text Articles in Medicinal-Pharmaceutical Chemistry

Development Of Single And Multimodality Imaging Probes For Pet, Spect And Fluorescence Imaging, Babak Behnam Azad Sep 2011

Development Of Single And Multimodality Imaging Probes For Pet, Spect And Fluorescence Imaging, Babak Behnam Azad

Electronic Thesis and Dissertation Repository

This dissertation is in an integrated format discussing three major projects centered around probe development. In the first project, novel metal-chelated and fluorinated GLP-1 derivatives were prepared all containing D-Ala-8, a modification known to improve resistance towards degradation by dipeptidyl-peptidase IV. The effect of increased distance between DOTA and the peptide chain was investigated using a spacer, in order to reduce steric effects imposed by DOTA. Placement of linker and DOTA moieties were varied within the GLP-1 sequence to test for optimal metal-complex location. Binding affinity of peptide derivatives was determined in vitro with CHO/GLP-1R cell line and shown ...


Nir-Emissive Polymersomal Markers For Molecular-Level Detection Of Metastasis, Wei Qi Aug 2011

Nir-Emissive Polymersomal Markers For Molecular-Level Detection Of Metastasis, Wei Qi

Publicly Accessible Penn Dissertations

Noninvasive imaging technologies, capable of visualizing early carcinoma or dormant or latent metastatic tumor cells and evaluating the efficacy of cancer therapies are becoming increasingly important. In this thesis, NIR-emissive polymersomes are engineered for optimal cellular uptake to enable fluorescence-based tumor targeting. A series of benzothiadiazole conjugated porphyrin oligomers with high emission dipole strength and exceptional large quantum yields in the NIR region are synthesized for optimized emissive output would be greatly enhanced. Furthermore, this thesis established for the first time a class of universal chemistry modification methods to directly attach antibody to polymersomes surface with very high antibody coupling ...


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 ...


Thermochemistry And Bond Energies Of Acetohydrazide, Amides And Cyclic Alkyl Ethers, Sumit Charaya May 2011

Thermochemistry And Bond Energies Of Acetohydrazide, Amides And Cyclic Alkyl Ethers, Sumit Charaya

Theses

Structure, thermochemical properties, bond energies and internal rotation potentials of Acetic Acid Hydrazide (CH3CONHNH2), Acetamide (CH3CONH2) and N-methyl Acetamide (CH3CONHCH3) and their radicals corresponding to loss of hydrogen atom have been studied. Gas phase standard enthalpies of formation and bond energies were calculated using the DFT methods B3LYP/6-31G(d,p), B3LYP/6-31G(2d,2p) and the composite CBS-QB3 methods employing a series of work reactions to further improve accuracy of the ΔHf°(298K). Molecular structures, vibration frequencies and internal rotor potentials were calculated at DFT level. The enthalpies of the parent molecules ...


Synthesis Towards Synthetic Adenosine Receptor, Rajni Gupta May 2011

Synthesis Towards Synthetic Adenosine Receptor, Rajni Gupta

Theses

Adenosine is a biologically important molecule as it acts as local modulator with cytoprotective function in the body. Adenosine accumulates in the extracellular space in response to metabolic stress and cell damage, and elevations in extracellular adenosine level are found in conditions like myocardial ischemia, hypoxia, inflammation and trauma. Its abnormal concentration therefore could be a marker of many diseases. Therefore determining its concentration can help understand the physiological state of the body. However its selective detection by synthetic receptors is not possible till date.

Efforts have been made here to design molecular tweezer for adenosine. Multistep synthesis was done ...


The Synthesis And Biological Evaluation Of Tamandarin B Analogs, Kenneth Lassen May 2011

The Synthesis And Biological Evaluation Of Tamandarin B Analogs, Kenneth Lassen

Publicly Accessible Penn Dissertations

The tamandarin and didemnins are a class of cyclodepsipeptides that have shown a wide range of biological activity. The didemnins have demonstrated antitumor, antiviral and immunosuppressive activity at low nano- and femtomolar levels. Didemnin B was the first marine natural product to enter clinical trials in humans in the United States. The structures of tamandarins A and B were reported in 2000 and possess almost identical structure and biological activity to didemnin B. These compounds have shown impressive biological activity and some progress has been made in establishing structure-activity relationships. However, their molecular mechanism of action is still unclear. The ...


Synthesis Of A Resveratrol Glycinate Derivative., Shelley Marie Van Cleve May 2011

Synthesis Of A Resveratrol Glycinate Derivative., Shelley Marie Van Cleve

Electronic Theses and Dissertations

Recently, the compound resveratrol has had media attention as an anti carcinogen. However, the bioavailability of resveratrol is low in the human system due to its hydrophobic nature. Therefore, it must be administered in high dosages to be effective. A plethora of derivatives have been synthesized that have the potential of resveratrol but sadly share low bioavailability. The first effort of this research was an attempt to produce a more hydrophilic ester of resveratrol. Failing this, the final product was synthesized using a glycine derivative to produce 4-[(1E)-2-(3,5-diacetyloxyphenyl)ethenyl]phenyl N-[(1,1-dimethylethoxy)carbonyl]-glycinate.


Mechanistic Study Of The Small Molecule Inhibitor Dx-52-1, Junru Cui May 2011

Mechanistic Study Of The Small Molecule Inhibitor Dx-52-1, Junru Cui

Master's Theses

Cell migration is a basic biological process that is fundamental to several normal and disease processes such as embryonic development, tissue repair, immune function, angiogenesis and cancer cell invasion and metastasis. Small organic molecules inhibiting cell migration can be used as both research probes and therapeutic agents. DX-52-1, a semisynthetic derivative of the natural product quinocarmycin (also known as quinocarcin), inhibits the migration of Madin-Darby canine kidney epithelial cells with nanomolar concentration. We have identified galectin-3, a multifunctional protein whose best-known function is its sugar binding ability, as a secondary target of DX-52-1 with functions in cell motility. In addition ...


Detection Of Protein By Microdrop Analysis, Yogeshkumar Radadiya Apr 2011

Detection Of Protein By Microdrop Analysis, Yogeshkumar Radadiya

All Capstone Projects

Analysis of protein depends particularly on protein concentration. Protein concentration measurement is the most important part in the research work to conduct protein-related studies. Although there are many methods available for this purpose, each method has certain limitations. The aim of the experiment is to develop either new or modified analytical method for the analysis and detection of protein using newly introduced micro-plate reader equipped with Take-3 microplate with the help of Gen-5 software. An ideal assay should be simple and easy to carry out. Another aspect to be taken into consideration are low inference, stability of measured components and ...