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Articles 1 - 19 of 19

Full-Text Articles in Medicinal-Pharmaceutical Chemistry

Synthesis Of A Sulfur Variant For Treatment Of Trypanosomiasis, Carlos Vera-Esquivel Mar 2019

Synthesis Of A Sulfur Variant For Treatment Of Trypanosomiasis, Carlos Vera-Esquivel

Student Research and Creative Activity Fair

Previous work in our lab has found diphenyl ether benzylamines showed a successful response with a micromolar concentration of our lead compound to treat the deadly Trypanosamiosis rhodesience. Furthermore, mammalian cell lines saw promising resistance towards damages. The goal of this study was to synthesize a diphenyl thio benzylamine variant. This variant was more active toward T. b. rhodesience but showed more toxicity to both rat 10 (IC50 mM) and human cell lines (HFF, HC-04, U-2 OS, and HEK293). The selectivity index (ratio of toxicity to activity in the same concentration units (SI)) varied from 55 ...


Glucosamine From Hydrolysis Of 3d Printing Chitosan For Osteoarthritis Treatment, Ruj Dansriboon, Laphon Premcharoen Jun 2018

Glucosamine From Hydrolysis Of 3d Printing Chitosan For Osteoarthritis Treatment, Ruj Dansriboon, Laphon Premcharoen

The International Student Science Fair 2018

This project aims to introduce a new way for osteoarthritis treatment which is expected to increase in the future. Glucosamine is the main subject for a treatment, which can be derived by hydrolyzing chitosan. This project also includes extraction of chitosan from shrimp waste to make a worthy use of food waste from industry. In this project, 3D printer is applied to print chitosan gel since 3D printing is adjustable to form various shapes of the gel.

The research process begins with the extraction of chitosan from shrimp shells. For the next step, the percent of deacetylation of chitosan was ...


A Novel Bromodomain And Extra-Terminal Domain Inhibitors (Beti) That Reverses Hiv-1 Latency, Shuai Liu, Maxime Jean, Wei Zhang, Jian Zhu May 2017

A Novel Bromodomain And Extra-Terminal Domain Inhibitors (Beti) That Reverses Hiv-1 Latency, Shuai Liu, Maxime Jean, Wei Zhang, Jian Zhu

UMass Center for Clinical and Translational Science Research Retreat

Although combinatory antiretroviral therapy (cART) is effective to reduce HIV-1 viremia, it does not eliminate HIV-1 infection. HIV-1 remains latent with the presence of cART, impeding the cure of AIDS. Recently, latency-reversing agents (LRAs) have been developed to purge latent HIV-1, providing an intriguing strategy for eradication of residual, latent viral reservoirs. Our earlier studies show that antagonism of HIV-1 competitive factor bromodomain containing 4 (BRD4) using bromodomain and extra-terminal domain inhibitor (BETi) JQ1 may facilitate the reversal of HIV-1 latency. BETis have recently emerged as a class of compounds that are promising for both the anticancer and HIV-1 latency-reversing ...


Docking Studies Of Isoform-Selectivity Of Phosphatidylinositol 3-Kinase (Pi3k) Inhibitors, Kaitlin Goettsch Mar 2017

Docking Studies Of Isoform-Selectivity Of Phosphatidylinositol 3-Kinase (Pi3k) Inhibitors, Kaitlin Goettsch

Student Research and Creative Activity Fair

Phosphatidylinositol 3-kinases (PI3Ks) and their related pathways are reputed targets for drug-based anticancer therapies. Mutations in PI3K genes, expression, and pathways are frequent among multiple cancer types. Four isoforms of PI3Ks exist: α, β, γ, & δ and studies have identified several ligands for each isoform which are capable of serving as inhibitory therapeutic compounds. However, the biochemical efficacy of these molecules varies and the isoform selectivity is not well understood. In this study, we applied in silico docking methods and free energy calculation methods to estimate the binding of reported PI3K ligands against 5 PI3K structures: PI3Kα (PBD ID: 2RD0 ...


Terpenes As ‘Resistance-Busting” Anthelmintic Drug, Zeynep Mirza, David Koch, Thanh-Thanh Nguyen, Yan Hu, Raffi V. Aroian, Gary R. Ostroff May 2016

Terpenes As ‘Resistance-Busting” Anthelmintic Drug, Zeynep Mirza, David Koch, Thanh-Thanh Nguyen, Yan Hu, Raffi V. Aroian, Gary R. Ostroff

UMass Center for Clinical and Translational Science Research Retreat

There is an urgent need for new therapies for parasitic helminthic diseases affecting 1.5-2 billion people worldwide due to the threat of wide-spread resistance development to existing treatments and due to problems of incomplete efficacies.

Terpenes are plant secondary metabolites and major essential oil constituents. Historically, the terpene thymol was successfully used to cure hookworm infections in the 1900’s. Although effective, large doses were needed and thymol treatment had significant side effects. Because free terpenes are absorbed in the stomach, less than 10% of oral terpenes entered the site where the parasites live. To overcome these problems we ...


Theoretical And Experimental Analysis Of The Antioxidant And Anti-Amyloid Features Of Synthetic Resveratrol Mimics, William Horton, Anne Kokel, Fanni Török, Chris Tran, Marianna Török, Bela Török May 2016

Theoretical And Experimental Analysis Of The Antioxidant And Anti-Amyloid Features Of Synthetic Resveratrol Mimics, William Horton, Anne Kokel, Fanni Török, Chris Tran, Marianna Török, Bela Török

UMass Center for Clinical and Translational Science Research Retreat

Diaryl hydrazones, possessing similar structure to the popular red wine antioxidant resveratrol, have been previously identified as multitarget compounds interfering with several processes associated with the pathogenesis of Alzheimer’s disease (AD). These compounds exhibited particularly strong inhibition of the amyloid beta (A) peptide self-assembly, including blocking the formation of fibrils and oligomers, species that are widely accepted to be neurotoxic. The molecules were also powerful free radical scavengers and thus have a potential to defend against oxidative stress.

In order to learn more about the mode of action of the compounds, theoretical and experimental studies have been carried out ...


Crystal Protein Cry5b As A Novel And Powerful Anthelmintic, David Koch, Zeynep Mirza, Yan Hu, Thanh-Thanh Nguyen, Gary R. Ostroff, Raffi V. Aroian May 2016

Crystal Protein Cry5b As A Novel And Powerful Anthelmintic, David Koch, Zeynep Mirza, Yan Hu, Thanh-Thanh Nguyen, Gary R. Ostroff, Raffi V. Aroian

UMass Center for Clinical and Translational Science Research Retreat

Soil-transmitted helminths (STHs), most notably, hookworms, whipworms, and Ascaris, are nematodes that infect more than 1.5 billion of the poorest people and are amongst the leading causes of morbidity worldwide. Only two classes of de-worming drugs (anthelmintics) are available for treatment, and only one is commonly used in mass drug administrations. New anthelmintics are urgently needed to overcome emerging resistance and to produce higher cure rates. Crystal (Cry) proteins, in particular Cry5B, made by Bacillus thuringiensis (Bt) are promising new candidates. Cry5B has excellent anthelmintic properties against many free-living and parasitic nematodes, including in vivo efficacy against multiple STH ...


Structural Activity Relationship Study On Dual Plk1 /Brd4 Inhibitor, Bi- 2536, Hailemichael Yosief, Shuai Liu, Dennis L. Buckley, Justin M. Roberts, Alex M. Muthengi, Francesca M. Corsini, James E. Bradner, Wei Zhang May 2016

Structural Activity Relationship Study On Dual Plk1 /Brd4 Inhibitor, Bi- 2536, Hailemichael Yosief, Shuai Liu, Dennis L. Buckley, Justin M. Roberts, Alex M. Muthengi, Francesca M. Corsini, James E. Bradner, Wei Zhang

UMass Center for Clinical and Translational Science Research Retreat

Polo-like kinase 1 (PLK1) and BRD4 are two different therapeutic targets in cancer drug discovery. Recently it has been reported that PLK1 inhibitor, BI-2536, is also a potent inhibitor of BRD4. The simultaneous inhibition of PLK1 and BRD4 by a single drug molecule is interesting because this could lead to the development of effective therapeutic strategy for different types of disease conditions in which PLK1 and BRD4 are implicated. Structural activity relationship studies has been carried out on BI-2536 to generate analogs with enhanced dual inhibitory activity against BRD4 and PLK1 as well as to render the molecule selective to ...


Comparison Of Conventional And Microwave-Assisted Synthesis Of Chemokine Receptor Type 4 (Cxcr4) Antagonists, Saniya Virani, Damilola Gbadebo, Theresa D. Gaines, Francisco Javier Garcia Apr 2016

Comparison Of Conventional And Microwave-Assisted Synthesis Of Chemokine Receptor Type 4 (Cxcr4) Antagonists, Saniya Virani, Damilola Gbadebo, Theresa D. Gaines, Francisco Javier Garcia

Georgia State Undergraduate Research Conference

No abstract provided.


Analysis Of New Hiv-1 Inhibitors As Potential Antiviral Agents For Hiv-2, Rowan Brothers Apr 2016

Analysis Of New Hiv-1 Inhibitors As Potential Antiviral Agents For Hiv-2, Rowan Brothers

Georgia State Undergraduate Research Conference

No abstract provided.


Electronic Cigarettes: Truth Or Toxic?, Timothy S. Turner, Alyx S. Frantzen Mar 2016

Electronic Cigarettes: Truth Or Toxic?, Timothy S. Turner, Alyx S. Frantzen

Undergraduate Research Conference

With the increasing research on the hazards of cigareDes, people are looking for a safer alterna>ve to smoking. Electronic CigareDes were introduced in the early 2000’s to serve this purpose, and they are gaining increasing popularity. Many e-cigareDe companies claim that the use of e-cigareDes is completely harmless because of combus>on of the organic liquids would cause the inhala>on of only water vapor and carbon dioxide along with the flavors and nico>ne. Companies also adver>se their products to help smokers quit smoking. Recently, “vaping” has grown increasingly popular especially with minors since several states ...


In Vivo Evaluation Of A Biomimetic Polymer-Doxorubicin Conjugate For Cancer Therapy, Matthew Skinner, Samantha Mcrae Page, Xiangji Chen, Sangram S. Parelkar, Kaitlyn Wong, Maria Mora, Sallie S. Schneider, Todd S. Emrick May 2014

In Vivo Evaluation Of A Biomimetic Polymer-Doxorubicin Conjugate For Cancer Therapy, Matthew Skinner, Samantha Mcrae Page, Xiangji Chen, Sangram S. Parelkar, Kaitlyn Wong, Maria Mora, Sallie S. Schneider, Todd S. Emrick

UMass Center for Clinical and Translational Science Research Retreat

This poster will describe a novel polymer pro-drug platform designed for conjugation and delivery of chemotherapeutics. Specifically, polymer pro-drugs were prepared from functional polymer zwitterions and doxorubicin (DOX), and evaluated in vivo to assess toxicological, pharmacokinetic and therapeutic properties. The biocompatible polymer scaffold (PolyMPC) consists of zwitterionic phosphorylcholine pendent groups, which mimic the natural hydrophilic moieties of phospholipids in cell membranes, and hydrazone linkages that allow for pH-triggered release of DOX. PolyMPC-DOX pro-drugs were isolated as dry solids using a facile strategy that allows for precise control of molecular weight and DOX incorporation. In vivo toxicity of PolyMPC and PolyMPC-DOX ...


Enhancing Antibiotic Activity Using Nanomaterial-Antibiotic Conjugates, H. Surangi N. Jayawardena, Thareendra De Zoysa, Kalana W. Jayawardana, Scott T. Boiko, Mingdi Yan May 2014

Enhancing Antibiotic Activity Using Nanomaterial-Antibiotic Conjugates, H. Surangi N. Jayawardena, Thareendra De Zoysa, Kalana W. Jayawardana, Scott T. Boiko, Mingdi Yan

UMass Center for Clinical and Translational Science Research Retreat

We demonstrate that streptomycin conjugated on silica nanoparticles (SNP-Str) can be used to effectively target streptomycin-resistant Escherichia coli (E. coli) bacteria by lowering the minimum inhibitory concentration (MIC) of streptomycin up to 2 log folds. Silica nanoparticles were synthesized with an average diameter of 80, 50 and 30 nm, respectively. Streptomycin was then covalently conjugated to SNP using efficient photocoupling chemistry. The MIC for free streptomycin sulfate was recorded as a high 2.0 mg/mL for an engineered Strr mutant E. coli ORN 208. Conjugating the streptomycin to SNP resulted in the decrease in MIC to 161 μg/mL ...


Interactions Of Carbohydrate-Conjugated Nanoparticles With Mycobacterium Smegmatis, Kalana W. Jayawardana, H. Surangi N. Jayawardena, Thareendra De Zoysa, Mingdi Yan May 2014

Interactions Of Carbohydrate-Conjugated Nanoparticles With Mycobacterium Smegmatis, Kalana W. Jayawardana, H. Surangi N. Jayawardena, Thareendra De Zoysa, Mingdi Yan

UMass Center for Clinical and Translational Science Research Retreat

Mycobacterium smegmatis is a non-pathogenic microorganism and has been widely used as a model organism to study infections caused by M. tuberculosis and other mycobacterial pathogens. We report that nanoparticles conjugated with selected carbohydrate show a striking increase in the surface adherence by M. smegmatis. This applies to silica nanoparticles and magnetic nanoparticles ranging from 100 nm to 5 nm. Under the same experimental conditions, minimum adhesion was observed for unfunctionalized nanoparticles. The synthesis and characterization of the glyconanoparticles will be presented. The finding is applied to imaging M. smegmatis infected lung epithelial cells, and the results will be discussed.


Application Of Diarylhydrazones, Schiff-Bases And Their Saturated Derivatives As Multifunctional Inhibitors Of Amyloid Self-Assembly, Christian Schafer, Sanjukta Ghosh, Marianna Torok, Bela Torok May 2014

Application Of Diarylhydrazones, Schiff-Bases And Their Saturated Derivatives As Multifunctional Inhibitors Of Amyloid Self-Assembly, Christian Schafer, Sanjukta Ghosh, Marianna Torok, Bela Torok

UMass Center for Clinical and Translational Science Research Retreat

A new class of multifunctional small molecule inhibitors of amyloid self-assembly is described. Several compounds, based on the diarylhydrazone scaffold were designed. Forty-four substituted derivatives of this core structure were synthesized using a variety of benzaldehydes and phenylhydrazines and were characterized. The inhibitor candidates were evaluated in multiple assays, including the inhibition of A fibrillogenesis and the disassembly of preformed fibrils. The hydrazone scaffold showed strong activity in inhibiting the amyloid beta self-assembly. The structure-activity relationship revealed that the substituents on the aromatic rings had considerable effect on the overall activity of the compounds. In order to identify possible functional ...


Synthesis Of Thiophene Analogs As Potential Antagonists Of Chemokine Receptor Type 4 (Cxcr4), Francisco Javier Garcia Jr. Apr 2014

Synthesis Of Thiophene Analogs As Potential Antagonists Of Chemokine Receptor Type 4 (Cxcr4), Francisco Javier Garcia Jr.

Georgia State Undergraduate Research Conference

No abstract provided.


Cell Migration Dynamics After Alteration Of Cell-Cell Contacts In Fibrosarcoma And Glioblastoma Cell Lines, Hassan S. Rizvi, Ronald K. Gary Aug 2011

Cell Migration Dynamics After Alteration Of Cell-Cell Contacts In Fibrosarcoma And Glioblastoma Cell Lines, Hassan S. Rizvi, Ronald K. Gary

Undergraduate Research Opportunities Program (UROP)

Cell migration is a vital component of metastasis. In this study, our intent was to study cell migration by alteration of the Wnt/GSK-3 Pathway. Since BeSO4 is a known GSK-3 kinase inhibitor, we hypothesized that this agent would cause cell migration to decrease as a result of β-catenin stabilization. Two human cell lines, HT-1080 (fibrosarcoma) and A172 (glioblastoma), were used to observe migration levels in the presence and absence of BeSO4. Our results show that cell migration is diminished for cells that were pre-treated with BeSO4, in comparison to the untreated (control) cells.


Synthesis Of Novel Aromatic Quinols For Colon And Renal Cancers, Bradley J. Davey, Tae Soo Jo, Pradip K. Bhowmik Aug 2010

Synthesis Of Novel Aromatic Quinols For Colon And Renal Cancers, Bradley J. Davey, Tae Soo Jo, Pradip K. Bhowmik

Undergraduate Research Opportunities Program (UROP)

Colon Cancer: The third most common cancer in USA. More than 1 million Americans currently living with colon cancer. 148,810 new cases expected in 2010. 50,000 deaths annually.

Renal Cancer: Approximately 58,000 people diagnosed in USA annually. Seventh most common cancer and tenth most common cause of cancer related death in men.

Aromatic quinols have demonstrated in vitro antitumor activity. Three heteroaromatic quinols show antitumor activity.


Synthesis Of Bis-Styrylbenzene Derivatives Via Wittig-Horner Reaction, Joseph K. Wray, Tae Soo Jo, Pradip K. Browmik Aug 2010

Synthesis Of Bis-Styrylbenzene Derivatives Via Wittig-Horner Reaction, Joseph K. Wray, Tae Soo Jo, Pradip K. Browmik

Undergraduate Research Opportunities Program (UROP)

Alzheimer’s Disease is now one of the most common diseases affecting the elderly population. Recently, bis-styrylbenzene derivatives have been shown to reduce the formation of Beta-amyloid plaques in the brain which are profoundly correlated with this disease. Finding new biologically active compounds which can reduce or prevent Alzheimer’s Disease has drawn much attention over the past few decades. Georg Wittig, Nobel Prize Winner in Chemistry, 1979.