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Spectral Properties Of Doxorubicin Doped Rhdl Nanoparticles, Sunil Shah 2018 University of North Texas Health Science Center at Fort Worth

Spectral Properties Of Doxorubicin Doped Rhdl Nanoparticles, Sunil Shah

Theses and Dissertations

Doxorubicin, also known as Adriamycin, is an anthracycline antibiotic which first gained clinical prominence in the early 1970’s as an effective antitumor agent. It is still used today to treat a spectrum of cancers like lymphoma, bladder, stomach, lung, breast, ovarian, and several others. Due to its production of free radicals to attack tumor cells, Doxorubicin interferes with mitochondrial phosphorylation and also induces cardiotoxicity. Thus, efficient and biocompatible delivery methods are needed for targeted drug delivery to overcome systemic toxicity. To maintain a high level of growth, tumor cells overexpress Scavenger receptors type B-1 (SR-B1). This cellular characteristic can ...


Catalyzed And Uncatalyzed Modifications Of Nucleosides, Synthesis Of Hippadine, And Deuterated 1,2,3-Triazoles, Hari K. Akula 2018 The Graduate Center, City University of New York

Catalyzed And Uncatalyzed Modifications Of Nucleosides, Synthesis Of Hippadine, And Deuterated 1,2,3-Triazoles, Hari K. Akula

All Dissertations, Theses, and Capstone Projects

The C4 amide carbonyl of O-t-butyldimethylsilyl-protected thymidine, 2’-deoxyuridine, and 3’-azidothymidine (AZT) was activated by reaction with (benzotriazol-1-yloxy)tris(dimethylamino) phosphonium hexafluorophosphate (BOP) and 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) in THF as solvent. This led to the formation of corresponding O4-(benzotriazol-1-yl) derivatives, which are reactive intermediates. Substitution at the C4 position was then carried out by reactions with alkyl and aryl amines, and thiols. Typically, reactions were conducted as a two-step, one-pot transformation, and also as a one-step conversion. After examining the reactions, the formation of 1-(4-pyrimidinyl)-1H-benzotriazole-3-oxide derivatives from the ...


C. Elegans Multidrug Resistance Protein 5 (Mrp-5) Transports Vitamin B12 From The Intestine To The Gonad To Support Embryonic Development, Huimin Na, Olga Ponomarova, Gabrielle E. Giese, Albertha J. M. Walhout 2018 University of Massachusetts Medical School

C. Elegans Multidrug Resistance Protein 5 (Mrp-5) Transports Vitamin B12 From The Intestine To The Gonad To Support Embryonic Development, Huimin Na, Olga Ponomarova, Gabrielle E. Giese, Albertha J. M. Walhout

University of Massachusetts Medical School Faculty Publications

Vitamin B12 functions as a cofactor for methionine synthase to produce the anabolic methyl donor S-adenosylmethionine (SAM) and for methylmalonyl-CoA mutase to catabolize the short chain fatty acid propionate. In the nematode Caenorhabditis elegans, maternally supplied vitamin B12 is required for the development of her offspring. However, the mechanism for exporting vitamin B12 from the mother to her offspring is not yet known. Here, we use RNAi of more than 200 transporters with a vitamin B12-sensor transgene to identify the ABC transporter MRP-5 as a candidate vitamin B12 exporter. We show that injection of vitamin B12 into the gonad of ...


Recently Discovered Benzo(A)Pyrene Induced Health Effects And Their Threat To The Inland Empire, Quinn Navarro 2018 University of Redlands

Recently Discovered Benzo(A)Pyrene Induced Health Effects And Their Threat To The Inland Empire, Quinn Navarro

Armacost Library Undergraduate Research Award (ALURA)

This study investigated recent discoveries of Benzo(a)Pyrene (BaP) in order to determine the current threat BaP poses to residents of Southern California. Literature reviews comprise the research done on BaP-induced health effects. Primary articles reviewed include “Adverse Effect of Sub-Chronic Exposure to Benzo(a)Pyrene and Protective Effect of Butylated Hydroxyanisole on Learning and Memory Ability in Male

Sprague-Dawley Rat” by Xiao Liang (2014), and “Bioaccumulation and oxidative damage in juvenile scallop Chlamys farreri exposed to benzo[a]Pyrene, benzo[b]Fluoranthene and chrysene” by Meng Xiu (2014). These studies conclude that BaP potentially impairs memory and learning ...


Diversity Oriented Synthesis, Characterization And Anti-Cancer Activity Of Killer Peptide Nucleolipid Bioconjugates, Niki K. Rana 2017 Seton Hall University

Diversity Oriented Synthesis, Characterization And Anti-Cancer Activity Of Killer Peptide Nucleolipid Bioconjugates, Niki K. Rana

Seton Hall University Dissertations and Theses (ETDs)

The killer peptide sequence D-(KLAKLAK)2 has been originally designed and developed as an antibacterial agent. Despite having excellent cytotoxicity towards bacteria, this sequence maintains low cell cytotoxity in malignant mammalian cell types such as cancer. The chemical basis for its selectivity has been attributed to its poly(cationic) amphiphilic nature, which facilitates cell permeability across the negatively charged bacterial membrane, but with limited permeability across the zwitterionic membrane of mammalian cells. The positively charged D-(KLAKLAK)2 sequence has been found to accumulate on the surface of the mitochondria causing dissipation of the negatively charged mitochondrial membrane potential ...


Structure Activity Relationship Studies Of Novel Diarylpentanoid Analogs Targeting The Androgen Receptor In Prostate Cancer Cells, Haili Coffin, Marco Bisoffi 2017 Chapman University

Structure Activity Relationship Studies Of Novel Diarylpentanoid Analogs Targeting The Androgen Receptor In Prostate Cancer Cells, Haili Coffin, Marco Bisoffi

Student Scholar Symposium Abstracts and Posters

The development of prostate cancer (PCa) relies strongly on the activation of the androgen receptor (AR) signaling pathway by its natural ligand dihydrotestosterone. Furthermore, PCa progression to metastatic disease represents oncogene addiction to AR activity. Androgen ablation therapy is thus a mainstay therapy against this disease, but the development of ligand-independent AR activation and persisting AR expression eventually leads to castration resistant PCa (CRPC). Therefore, down-regulation of AR expression in PCa cells may be an effective therapeutic modality. The diarylpentanoid ca27 has previously been shown to down-regulate AR expression by an unknown mechanism of action. The present work represents a ...


Synthesis Of Aza-Tetracyclic Indolines For The Treatment Of Methicillin-Resistant Staphylococcus Aureus, Kevin Xie 2017 University of Colorado, Boulder

Synthesis Of Aza-Tetracyclic Indolines For The Treatment Of Methicillin-Resistant Staphylococcus Aureus, Kevin Xie

Undergraduate Honors Theses

Antibiotic resistance is a major threat to public health. Currently new multi-drug resistant bacterial strains are appearing faster than new antibiotics can enter the clinic. Resistance modifying agents can potentially potentiate whole families of antibiotics and are one way to combat antibiotic resistance. Previously, our lab synthesized a library of polycyclic indolines which were found to potentiate β-lactams in MRSA in vitro but were poor candidates for in vivo testing due to their physical properties. To improve their physical properties, we synthesized a small library of aza-tetracyclic indolines. The nitrogen was functionalized with various functional groups to determine which modifications ...


A Diversity-Oriented Synthesis Approach To Functionalized Azaheterocycles Using Cyclic Alpha-Halo Eneformamides, Spencer A. Langevin 2017 Central Washington University

A Diversity-Oriented Synthesis Approach To Functionalized Azaheterocycles Using Cyclic Alpha-Halo Eneformamides, Spencer A. Langevin

All Master's Theses

Functionalized piperidines, azepanes, azamacrocycles, morpholines, and thiomorpholines are common structural motifs found in a wide range of pharmaceuticals such as carmegliptine, levofloxacin, thioridazine, claviciptic acid, and azithomycin. As a result, there is a strong desire to construct highly functionalized nitrogen-bearing ring scaffolds in order to construct a wide range of drug possibilities. There are several non-modular and step-uneconomical synthetic methods used in the construction of these aforementioned motifs such as ring closing metathesis, ring expansions, and intramolecular reductive amination. In this research, we present a step-economical, cost-effective, scalable, and diversity-oriented synthesis approach to highly functionalized N-heterocycles through the intermediacy of ...


Chemoselective And Stereoselective Exploration Of The Chemical Reactivity Space Of Castagnoli-Cushman-Derived Allylic Lactamoyl Esters: Application To The Synthesis Of Aza-Polycylic Architectures, Brandon Joseph Mansker 2017 Central Washington University

Chemoselective And Stereoselective Exploration Of The Chemical Reactivity Space Of Castagnoli-Cushman-Derived Allylic Lactamoyl Esters: Application To The Synthesis Of Aza-Polycylic Architectures, Brandon Joseph Mansker

All Master's Theses

The synthesis and evaluation of structure-activity relationships of saturated nitrogen heterocycles is the focal point of various pharmaceutical companies thanks to the high biological activity of previously isolated azacycles. Here, we describe an operationally simple and highly efficient approach to macrocyclic lactams bearing vicinal stereocenters and a challenging cycloalkyne motif. The outcomes are achieved through a novel [4 + 2] cycloaddition reaction between an N-iodoarylated-1,3-azadiene and cyclic anhydrides, followed by interception of the cycloadducts in cross-coupling manifolds (e.g., Sonogashira coupling) and concomitant lithiation-cyclization of the tethered alkyne. An unprecedented example of a hydroamino alkylation that is transition metal-free ...


An Evaluation Of Antibiotic Resistance: Structure-Activity Relationship Studies Of Tetracyclic Indolines As A Novel Class Of Resistance-Modifying Agents For Mrsa & Analysis Of Recent Fda Regulations On Antibiotic Use In Livestock, Lakota K. Cleaver 2016 University of Colorado, Boulder

An Evaluation Of Antibiotic Resistance: Structure-Activity Relationship Studies Of Tetracyclic Indolines As A Novel Class Of Resistance-Modifying Agents For Mrsa & Analysis Of Recent Fda Regulations On Antibiotic Use In Livestock, Lakota K. Cleaver

Undergraduate Honors Theses

While the rate at which resistance develops against antimicrobials rises, research and development for new antimicrobials declines. By placing selective pressure on bacteria we are inadvertently forcing bacteria into expressing and propagating genes conferring high levels of resistance. Continued misuse and overuse of antibiotics, in light of the evident problem developing, must be resolved. To find a resolve, a multidisciplinary and multifaceted approach must be taken which involves 1) research and development of novel antimicrobial agents and 2) governmental regulation.

Strides in new antimicrobial drug development largely revolve around making old antibiotics usable again. Resistance-Modifying Agents (RMAs) act to re-sensitize ...


Testosterone Treatment Does Not Facilitate Prefrontal Cortex Mediated Cognition In Male Marmosets (Callithrix Jacchus), Matthew LaClair, Jeemin Chang, Agnes Lacreuse 2015 University of Massachusetts Amherst

Testosterone Treatment Does Not Facilitate Prefrontal Cortex Mediated Cognition In Male Marmosets (Callithrix Jacchus), Matthew Laclair, Jeemin Chang, Agnes Lacreuse

Agnes Lacreuse

Aging in men is associated with decreases in serum testosterone (T) and a decline in cognitive abilities. We sought to clarify the relationship between T, aging and cognition using the common marmoset (callithrix jacchus), which has been shown to be a useful model of human aging. Ten castrated male marmosets (ages 3-8) were given weekly injections of either T cypionate dissolved in cottonseed oil (T, n = 5) or cottonseed oil alone (controls, n = 5). Cognitive function was assessed with two tasks, the object reversals (OR) and the delayed response (DR). Marmoset behavior was recorded twice daily using a modified frequency ...


Synthesis Of Β-Triphosphotriester Pronucleotides, Yousef A. Beni, Chandravanu Dash, Keykavous Parang 2015 Tennessee State University

Synthesis Of Β-Triphosphotriester Pronucleotides, Yousef A. Beni, Chandravanu Dash, Keykavous Parang

Pharmacy Faculty Articles and Research

Dinucleoside phosphorochloridite were synthesized from phosphorus trichloride and three nucleoside analogues, 3-fluoro-2,3-dideoxythymidine (FLT), 2',3'-dideoxy-5-fluoro-3'- thiacytidine (FTC), and 2',3'-dideoxy-3'-thiacytidine (3TC), in a multistep synthesis. Polymerbound N-Boc p-acetoxybenzyl 5¢-O-2¢-deoxythymidine was reacted with dinucleoside phosphorochloridite in the presence of 2,6-lutidine, followed by the reaction with dodecyl alcohol and 5-(ethylthio)-1H-tetrazole, oxidation with tert-butyl hydroperoxide, and acidic cleavage, respectively, to afford the b-triphosphotriester derivatives containing three different nucleosides.


Target-Directed Biosynthetic Evolution: Redirecting Plant Evolution To Genomically Optimize A Plant’S Pharmacological Profile, Dustin Paul Brown 2015 University of Kentucky

Target-Directed Biosynthetic Evolution: Redirecting Plant Evolution To Genomically Optimize A Plant’S Pharmacological Profile, Dustin Paul Brown

Theses and Dissertations--Neuroscience

The dissertation describes a novel method for plant drug discovery based on mutation and selection of plant cells. Despite the industry focus on chemical synthesis, plants remain a source of potent and complex bioactive metabolites. Many of these have evolved as defensive compounds targeted on key proteins in the CNS of herbivorous insects, for example the insect dopamine transporter (DAT). Because of homology with the human DAT protein some of these metabolites have high abuse potential, but others may be valuable in treating drug dependence. This dissertation redirects the evolution of a native Lobelia species toward metabolites with greater activity ...


Testosterone Treatment Does Not Facilitate Prefrontal Cortex Mediated Cognition In Male Marmosets (Callithrix Jacchus), Matthew LaClair, Jeemin Chang, Agnes Lacreuse 2014 University of Massachusetts Amherst

Testosterone Treatment Does Not Facilitate Prefrontal Cortex Mediated Cognition In Male Marmosets (Callithrix Jacchus), Matthew Laclair, Jeemin Chang, Agnes Lacreuse

UMass Center for Clinical and Translational Science Research Retreat

Aging in men is associated with decreases in serum testosterone (T) and a decline in cognitive abilities. We sought to clarify the relationship between T, aging and cognition using the common marmoset (callithrix jacchus), which has been shown to be a useful model of human aging. Ten castrated male marmosets (ages 3-8) were given weekly injections of either T cypionate dissolved in cottonseed oil (T, n = 5) or cottonseed oil alone (controls, n = 5). Cognitive function was assessed with two tasks, the object reversals (OR) and the delayed response (DR). Marmoset behavior was recorded twice daily using a modified frequency ...


Polypharmacy In Elderly: A Cautious Trail To Tread, Saniya Raghib Sabzwari, Waris Qidwai, Seema Bhanji 2013 Aga Khan University

Polypharmacy In Elderly: A Cautious Trail To Tread, Saniya Raghib Sabzwari, Waris Qidwai, Seema Bhanji

Department of Family Medicine

Polypharmacy has now increasingly come into focus as the recipient of healthcare in old age worldwide. In elderly it is associated with frequent adverse drug reactions (ADRs) and drug-drug interactions resulting in significant morbidity. Geriatrics is still an emerging specialty in South Asia, especially in Pakistan, where multiple reasons for polypharmacy exist. An extensive literature review of articles using key words like \'polypharmacy,\' \'elderly\' was conducted. The recently updated Beers Criteria of classification of inappropriate drugs in the elderly was reviewed in detail. Articles of relevance to polypharmacy and evaluation of guidelines for appropriate interventions to minimise inappropriate drug prescribing ...


Developing Pentamethine Cyanine Dyes For Photodynamic Therapy, Quoc Bao H. Nguyen 2013 Georgia State University

Developing Pentamethine Cyanine Dyes For Photodynamic Therapy, Quoc Bao H. Nguyen

Georgia State Undergraduate Research Conference

No abstract provided.


Asymmetric Total Synthesis Of Congeners Of Hydramycin, An Anthraquinone-Type Antitumor Agent, Costyl Ngnouomeuchi Njiojob 2013 Selected Works

Asymmetric Total Synthesis Of Congeners Of Hydramycin, An Anthraquinone-Type Antitumor Agent, Costyl Ngnouomeuchi Njiojob

Costyl Ngnouomeuchi Njiojob

Hydramycin is an antitumor antibiotic isolated from Streptomyces violaceus. It is a pyranoanthraquinone-type antitumor agent that has shown broad-spectrum activity against a variety of human-derived cancer cell lines. Among tumors evaluated at the National Cancer Institute (lung, colon, melanoma, breast and prostate), GI50s were <10−10 M in the NCI's 60-cell-line panel. We embarked on the synthesis and evaluation of a simplified congener 2-(1-hydroxy-1-(oxiran-2-yl)ethyl)-4H-naphtho[2,3-h]chromene-4,7,12-trione(17), which would facilitate synthesis while retaining the potent activity. Hydramycin has two chiral centers, and our goal is to design and synthesize all the possible ...


Asymmetric Total Synthesis Of Congeners Of Hydramycin, An Anthraquinone-Type Antitumor Agent, Costyl Ngnouomeuchi Njiojob 2011 University of Tennessee, Knoxville

Asymmetric Total Synthesis Of Congeners Of Hydramycin, An Anthraquinone-Type Antitumor Agent, Costyl Ngnouomeuchi Njiojob

Doctoral Dissertations

Hydramycin is an antitumor antibiotic isolated from Streptomyces violaceus. It is a pyranoanthraquinone-type antitumor agent that has shown broad-spectrum activity against a variety of human-derived cancer cell lines. Among tumors evaluated at the National Cancer Institute (lung, colon, melanoma, breast and prostate), GI50s were <10−10 M in the NCI's 60-cell-line panel. We embarked on the synthesis and evaluation of a simplified congener 2-(1-hydroxy-1-(oxiran-2-yl)ethyl)-4H-naphtho[2,3-h]chromene-4,7,12-trione(17), which would facilitate synthesis while retaining the potent activity. Hydramycin has two chiral centers, and our goal is to design and ...


What Is New For An Old Molecule? Systematic Review And Recommendations On The Use Of Resveratrol, Ole Vang, Nihal Ahmad, Karen Brown, Anna Csiszar, Thomas Szekeres, Thomas Walle, Joseph M. Wu 2011 New York Medical College

What Is New For An Old Molecule? Systematic Review And Recommendations On The Use Of Resveratrol, Ole Vang, Nihal Ahmad, Karen Brown, Anna Csiszar, Thomas Szekeres, Thomas Walle, Joseph M. Wu

NYMC Faculty Publications

BACKGROUND: Resveratrol is a natural compound suggested to have beneficial health effects. However, people are consuming resveratrol for this reason without having the adequate scientific evidence for its effects in humans. Therefore, scientific valid recommendations concerning the human intake of resveratrol based on available published scientific data are necessary. Such recommendations were formulated after the Resveratrol 2010 conference, held in September 2010 in Helsingør, Denmark.

METHODOLOGY: Literature search in databases as PUBMED and ISI Web of Science in combination with manual search was used to answer the following five questions: (1)Can resveratrol be recommended in the prevention or treatment ...


A Global Analysis Of The Adaptations Required For Sterol Catabolism In Mycobacterium Tuberculosis: A Dissertation, Jennifer E. Griffin 2011 University of Massachusetts Medical School

A Global Analysis Of The Adaptations Required For Sterol Catabolism In Mycobacterium Tuberculosis: A Dissertation, Jennifer E. Griffin

GSBS Dissertations and Theses

Systems biology approaches have allowed for comprehensive understanding of complicated biological processes. Here, we’ve developed a global phenotypic profiling method by improving upon transposon mutagenesis methods for identifying genes required for bacterial growth in various conditions. By using the massively parallel power of Illumina sequencing, we precisely redefined the genes required for the growth of Mycobacterium Tuberculosis (Mtb) in vitro. This adapted technique provided more informative data with both increased dynamic range and resolution. As a result, we quantitatively assessed the fitness of individual mutants, as well as identified sub-genic essentiality. Mtb is well adapted to its nutrient-limiting intracellular ...


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