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Articles 31 - 53 of 53

Full-Text Articles in Organic Chemistry

Synthesis And Characterization Of Imidazolium Salt Derivatives For Anti-Tumor Activity, Ryan W. Pearce Jan 2015

Synthesis And Characterization Of Imidazolium Salt Derivatives For Anti-Tumor Activity, Ryan W. Pearce

Williams Honors College, Honors Research Projects

Several aldehydes (butanal, pentanal, hexanal, 4-hydroxybenzaldehyde) were reacted with 1,3-bis(naphthalen-2-ylmethyl)-imidazolium bromide (1) to produce novel C2 substituted imidazolium salts for the potential use against non-small cell lung cancer in humans. Compounds 2-(1-hydroxypentyl)-1,3-bis(naphthalen-2-ylmethyl)-imidazolium bromide (3) and 2-(1-hydroxyhexyl)-1,3-bis(naphthalen-2-ylmethyl)-imidazolium bromide (5) were successfully synthesized with structures supported by NMR and mass spectrometry. Characterization by 1H NMR showed evidence of 1 in both compounds. The tumor cell growth inhibition of 3 against non-small cell lung cancer lines NCI-A549, NCI-H460, HCC827, and NCI-H1975 was tested and found to be comparable ...


Chemoenzymatic Studies To Enhance The Chemical Space Of Natural Products, Jhong-Min Chen Jan 2015

Chemoenzymatic Studies To Enhance The Chemical Space Of Natural Products, Jhong-Min Chen

Theses and Dissertations--Pharmacy

Natural products provide some of the most potent anticancer agents and offer a template for new drug design or improvement with the advantage of an enormous chemical space. The overall goal of this thesis research is to enhance the chemical space of two natural products in order to generate novel drugs with better in vivo bioactivities than the original natural products.

Polycarcin V (PV) is a gilvocarcin-type antitumor agent with similar structure and comparable bioactivity with the principle compound of this group, gilvocarcin V (GV). Modest modifications of the polyketide-derived tetracyclic core of GV had been accomplished, but the most ...


Design, Synthesis And Biological Evaluation Of Novel Compounds With Cns-Activity Targeting Cannabinoid And Biogenic Amine Receptors, Alexander M. Sherwood May 2014

Design, Synthesis And Biological Evaluation Of Novel Compounds With Cns-Activity Targeting Cannabinoid And Biogenic Amine Receptors, Alexander M. Sherwood

University of New Orleans Theses and Dissertations

This work seeks to contribute to the discipline of neuropharmacology by way of structure activity relationship from the standpoint of an organic chemist. More specifically, we sought to develop robust synthetic methodology able to efficiently produce an array of compounds for the purpose of systematic evaluation of their interaction with specific sights within the central nervous system (CNS) in order to better understand the mind and to develop drugs that may have beneficial effects on neurological function.

The focus of these studies has been toward the development of novel molecules, using a structure-activity relationship approach, that exhibit binding affinity at ...


Functionalization And Modification Of Naphthaquinone Analogs As Her2 Kinase Inhibitors, Divya Jyothi Lella May 2014

Functionalization And Modification Of Naphthaquinone Analogs As Her2 Kinase Inhibitors, Divya Jyothi Lella

Masters Theses & Specialist Projects

HER2 overexpression in breast cancer tumors predicts lower overall survival. Because of the aggressive nature of HER2 tumors and the association with metastatic disease, the HER2 receptor holds great promise as a therapeutic target in metastatic breast cancer. We are developing small molecule inhibitors that bind to the ATP binding site of the tyrosine kinase domain in order to inhibit tyrosine auto-phosphorylation. This process controls biological pathways that mediate the cell growth. In normal cells this process is highly controlled. We are targeting the modification of the side chain of the hydroxy methyl group of 2-Hydroxy methyl-5,8-dimethoxy-1,4-naphthaquinone. These ...


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.


Development Of A Safe And Efficient Near-Infrared Diagnostic Method For Alzheimer's Disease, Joseph Tawney Apr 2014

Development Of A Safe And Efficient Near-Infrared Diagnostic Method For Alzheimer's Disease, Joseph Tawney

Georgia State Undergraduate Research Conference

No abstract provided.


Ligand-Receptor Interactions For Supramolecular Disassembly With Applications In Screening And Drug Delivery, Diego Amado Torres Jan 2014

Ligand-Receptor Interactions For Supramolecular Disassembly With Applications In Screening And Drug Delivery, Diego Amado Torres

Doctoral Dissertations

Proteins have the capacity to bind specific sets of compounds known as ligands, these are small molecules with a recurrent theme in their molecular design that is a characteristic exploited here to (i) identify particular affinities of small molecules for proteins with the aim of using them as ligands, inhibitors, or targeting moieties in more complex systems by means of a methodology that screens small molecules based on protein affinity; (ii) decorate a self-assembling supramolecular system at different positions, making it responsive to a complementary protein with the aim of exploring differences in disassembly and sensitivity of the release of ...


A New Methodology For The Synthesis Of 2-Alkyl-5,6-Bis(Alkylthio)Benzo[D]Thiazole-4,7-Dione, Jeena Foronda Jan 2014

A New Methodology For The Synthesis Of 2-Alkyl-5,6-Bis(Alkylthio)Benzo[D]Thiazole-4,7-Dione, Jeena Foronda

Senior Research Projects

Cancer is a rapidly growing fatal disease and with the various thiazole compounds being scientifically generated, possible treatment options can be implemented. Proper synthesis of 2,3-dimethoxy-1,4-benzoquinone allows for a variety of compounds to be made with further treatment of alkylthio reagents. Both thioacetamide and thiobenzamide are used to react with 2,3-dimethoxy-1,4-benzoquinone in order to build a library of thiazoles. Final compounds can be tested for the ability to inhibit recombinant enzyme activity and the capability to kill tumor cells. A basic oxidation procedure along with nucleophilic attack was used to create target products.


Design And Synthesis Of Novel Sultams As Non-Nucleoside Inhibitors Of Hiv Reverse Transcriptase, Brian Chadwick Lecroix Dec 2013

Design And Synthesis Of Novel Sultams As Non-Nucleoside Inhibitors Of Hiv Reverse Transcriptase, Brian Chadwick Lecroix

Doctoral Dissertations

The compound 2-methyl-3-phenyl-2,3-dihydro-1,2-benzisothiazole 1,1-dioxide (NSC 108406) was identified as an HIV-1 reverse transcriptase inhibitor by the National Cancer Institute. Using this lead, the Baker group has developed a series of analogues with various groups at the 3-position that show a spectrum of biological activities. In the end, the substituents used could not compare to the biological activity of the inhibitor efavirenz (Sustiva® [trademark]), and so it was decided to synthesize sultams with alkylethynyl substituents at the 3-position of the sultams in an attempt to mimic the activity of efavirenz.

Previous research analyzed the proposed novel sultams in ...


Developing A Presumptive Test For Select Synthetic Cannabinoids, Carrie Snyder Dec 2013

Developing A Presumptive Test For Select Synthetic Cannabinoids, Carrie Snyder

Theses and Dissertations

Synthetic cannabinoids (SC's) began to gain popularity around the world in 2009. Since then, many of the compounds have been outlawed and methods developed to detect them and their metabolites using mass spectrometry. Our work investigated the possibility of developing a colorimetric presumptive test. The SC JWH-019 was synthesized and its ketone targeted as a possible reaction site. Many SC's contain ketones and thus a reaction at this site would be applicable to many of the compounds. Since JWH-019 is costly and time consuming to synthesize, much of the experimental work was done using benzophenone (BP). BP contains ...


Comparison Of Methodologies For Synthesis Of 3-(Cyclopropylethynyl)Benzisothiazole 1,1-Dioxide, Rachel Lee Naramore May 2013

Comparison Of Methodologies For Synthesis Of 3-(Cyclopropylethynyl)Benzisothiazole 1,1-Dioxide, Rachel Lee Naramore

Chancellor’s Honors Program Projects

No abstract provided.


The Reaction Of Methionine With A Non-C2-Symmetrical Platinum (Ii) Diamine Compound, Nilesh Sahi May 2012

The Reaction Of Methionine With A Non-C2-Symmetrical Platinum (Ii) Diamine Compound, Nilesh Sahi

Honors College Capstone Experience/Thesis Projects

The research that we have conducted has allowed us to discover that the amino acids, methionine (Met) and N-acetyl methionine (N-AcMet), will react in a 1:1 and 1:2 molar ratio with platinum complexes containing bulky diamine ligands. Previous research has allowed us to gain a plethora of information on the experimentation and results of specific bulky diamine ligands such as N,N,N',N'-tetramethylethylenediamine and N,N-diethylethylenediamine. In the current study, we have investigated the bulky diamine ligand of N,N-dimethylethylenediamine, or Me2en. With our focus on the bulk of the Me2en ligand ...


Oxaliplatin And Oxaliplatin Derivatives: Synthesis, Characterization, And Reactivity With Biologically Relevant Ligands, Amy Poynter May 2012

Oxaliplatin And Oxaliplatin Derivatives: Synthesis, Characterization, And Reactivity With Biologically Relevant Ligands, Amy Poynter

Honors College Capstone Experience/Thesis Projects

Oxaliplatin is a third generation anticancer drug that has proven to be successful in fighting ovarian and testicular cancer. We are interested in determining how oxaliplatin and oxaliplatin derivatives interact with proteins, as well as how that interaction is affected by the size and shape of these platinum compounds. We have synthesized oxaliplatin as it is used in cancer treatment, as well as similar platinum compounds with the same diaminocyclohexane ligand as oxaliplatin but with additional bulk added to the nitrogen atoms. We are reacting oxaliplatin with key amino acids, including methionine, and will be comparing the kinetics of this ...


Ferrocene Constrained Helical Peptides Via On-Resin Cyclization, Thomas A. Mcteague Apr 2012

Ferrocene Constrained Helical Peptides Via On-Resin Cyclization, Thomas A. Mcteague

Senior Theses and Projects

Previous research within the Curran group has demonstrated that ferrocene may be used as an organometallic constraint to induce the formation of α-helices in short peptides which traditionally possess undefined conformations. Through strategic placement of lysine residues at the i and i+3 positions within the peptide, such a constraint was accomplished via the crosslinking of the lysine side chains to ferrocene dicarboxylic acid chloride in solution phase synthesis. The aim of this work was to develop a method for solid phase peptide synthesis (SPPS) for the synthesis of these ferrocene-constrained helices. In particular, we seek to develop a method ...


Polymers Used In Medicine: Common Types And Benefits Of Drug Delivery Systems, Camille Andrews Jan 2012

Polymers Used In Medicine: Common Types And Benefits Of Drug Delivery Systems, Camille Andrews

Natural Sciences Poster Sessions

This poster describes the common types and benefits of drug delivery systems.


Linus Pauling: Scientist Of The 20th Century, Laura Ward Jan 2012

Linus Pauling: Scientist Of The 20th Century, Laura Ward

Natural Sciences Poster Sessions

This poster describes the contributions scientist Linus Pauling made to the fields of chemistry and molecular biology, including his hybridization theory.


Parallel Text Immersion, Daniel P. Becker Ph.D. Dec 2011

Parallel Text Immersion, Daniel P. Becker Ph.D.

Daniel P. Becker

A new method of teaching foreign languages to beginning, intermediate, and advancing foreign language students is proposed involving reading out loud passages, chapters, and entire works of literature that are familiar to the student through required pre-reading in the students’ mother tongue. Testing is proposed to evaluate the success of the method.


Design And Syntheses Of Fluorescent Cytosine Analogues, David W. Dodd Apr 2011

Design And Syntheses Of Fluorescent Cytosine Analogues, David W. Dodd

Electronic Thesis and Dissertation Repository

The avid hybridization of peptide nucleic acid (PNA) to DNA and RNA along with the molecule’s biological stability has led it to be used in both antisense and antigene capacities. PNA acts against translation via a steric blockade mechanism. It is therefore reasonable to assume that increased heteroduplex stability could lead to increased potency. Two ways of doing this were explored. I) N-Terminal attachment of a platinous chloride chelating moiety to PNA complementary to Xenopus noggin was synthesized with the objective of selective, covalent platination of the target transcript in vivo. Phenotypes consistent with knockdown of the selected ...


Β-Hetero Vinylzinc Reagents: Versatile Precursors For A Broad Spectrum Of High Impact Chemicals, Petr Valenta Dec 2010

Β-Hetero Vinylzinc Reagents: Versatile Precursors For A Broad Spectrum Of High Impact Chemicals, Petr Valenta

Publicly Accessible Penn Dissertations

Tandem methods for the catalytic asymmetric preparation of enantioenriched β-hydroxy (E)-enamines and cyclopropylamines are presented. The diastereoselective hydrogenation of enantioenriched (E)-trisubstituted hydroxy enamines to generate 1,2-disubstituted 1,3-amino alcohols is also outlined. These methods are initiated by highly regioselective hydroboration of N-tosyl substituted ynamides with diethylborane to generate β-amino alkenyl boranes. In situ boron to zinc transmetalation generates β-amino alkenyl zinc reagents. These functionalized vinylzinc intermediates were subsequently added to aldehydes in the presence of catalyst derived from an enantioenriched amino alcohol (morpholino isoborneol, MIB). The catalyst promotes highly enantioselective C–C bond-formation to provide β-hydroxy enamines ...


Coupling Coherence Distinguishes Structure Sensitivity In Protein Electron Transfer, Tatiana Prytkova, Igor V. Kurnikov, David Beratan Jan 2007

Coupling Coherence Distinguishes Structure Sensitivity In Protein Electron Transfer, Tatiana Prytkova, Igor V. Kurnikov, David Beratan

Biology, Chemistry, and Environmental Sciences Faculty Articles and Research

Quantum mechanical analysis of electron tunneling in nine thermally fluctuating cytochrome b562 derivatives reveals two distinct protein-mediated coupling limits. A structure-insensitive regime arises for redox partners coupled through dynamically averaged multiple-coupling pathways (in seven of the nine derivatives) where heme-edge coupling leads to the multiple-pathway regime. A structure-dependent limit governs redox partners coupled through a dominant pathway (in two of the nine derivatives) where axial-ligand coupling generates the single-pathway limit and slower rates. This two-regime paradigm provides a unified description of electron transfer rates in 26 ruthenium-modified heme and blue-copper proteins, as well as in numerous photosynthetic proteins.


Flavin Charge Transfer Transitions Assist Dna Photolyase Electron Transfer, Spiros S. Skourtis, Tatiana Prytkova, David Beratan Jan 2007

Flavin Charge Transfer Transitions Assist Dna Photolyase Electron Transfer, Spiros S. Skourtis, Tatiana Prytkova, David Beratan

Biology, Chemistry, and Environmental Sciences Faculty Articles and Research

This contribution describes molecular dynamics, semi-empirical and ab-initio studies of the primary photo-induced electron transfer reaction in DNA photolyase. DNA photolyases are FADH−-containing proteins that repair UV-damaged DNA by photo-induced electron transfer. A DNA photolyase recognizes and binds to cyclobutatne pyrimidine dimer lesions of DNA. The protein repairs a bound lesion by transferring an electron to the lesion from FADH−, upon photo-excitation of FADH− with 350–450 nm light. We compute the lowest singlet excited states of FADH− in DNA photolyase using INDO/S configuration interaction, time-dependent density-functional, and time-dependent Hartree-Fock methods. The calculations identify the lowest singlet excited ...


Pyrene Labeled Poly(Aryl Ether) Monodendrons: Synthesis, Characterization, Diffusion Coefficients, And Photophysical Studies, James Hanson, Jeanne Riley, Sibel Alkan, Wajiha Khan, Wyatt Murphy, Aidi Chen, Michael Shapiro Dec 2000

Pyrene Labeled Poly(Aryl Ether) Monodendrons: Synthesis, Characterization, Diffusion Coefficients, And Photophysical Studies, James Hanson, Jeanne Riley, Sibel Alkan, Wajiha Khan, Wyatt Murphy, Aidi Chen, Michael Shapiro

Wyatt Murphy

Four generations of poly(aryl ether) monodendrons labeled with pyrene at the focus were synthesized and characterized by a combination of NMR, size-exclusion chromatography with light scattering detection (SEC-LS), and electronic spectroscopy. The monodendrons were then studied by magnetic resonance and fluorescence techniques. Translational diffusion coefficients in THF-d8, acetonitrile-d3, and cyclohexane-d12 were measured by Pulsed-Field-Gradient NMR and ranged from 2.2 x 10-5 cm2/sec for methoxypyrene in acetonitrile to 3.4 x 10-6 cm2/sec for the fourth generation monodendron in THF. Molecular radii were calculated from the diffusion coefficients by the Stokes-Einstein equation. In THF, the radii increased ...


Solid Phase Peptide Synthesis, John Gibson Oct 1974

Solid Phase Peptide Synthesis, John Gibson

Honors Theses

Solid phase peptide synthesis is a relatively new biochemical process for polymerization of amino acids. It involves the selection of amino acids, blocking groups, and resins. This procedure was first investigated by R. B. Merrifield in an attempt to simplify previous methods of peptide synthesis. Since other methods involved amino acids, peptide esters, and diketopiperazines, peptide synthesis had been limited by amino acid selection and a host of technical problems. Solid phase synthesis alleviates many of these difficulties and limitations by supplying a faster and simpler stepwise addition of a wide variety of naturally occurring and synthetically prepared amino acids ...