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Articles 421 - 450 of 1033
Full-Text Articles in Chemistry
Interaction Of A Platinum Triamine Complex Having A Seven-Membered Chelate Ring With N-Acetyl-Lmethionine And Guanosine 5'-Monophosphate, Jae Ko
Masters Theses & Specialist Projects
In the 1960s, Rosenberg and his colleagues confirmed the anti-cancer activity of cisplatin. Although cisplatin was capable of killing testicular cancer cells there were also serious side effects. It was necessary to find alternate ways of overcoming side effects, and soon many researchers have discovered novel platinum compounds that show similar reactivity. Recently, replacing one chloride group to a heterocyclic amine group showed significant cytotoxicity with a different binding activity than cisplatin. Previously in our lab, [Pt(Me5dien)(NO3)]+ and [Pt(Et2dien)Cl]+ have been synthesized and reacted with NAcetyl- L-methionine (N-AcMet) and Guanosine 5’-monophosphate (5’-GMP) showed unusual reactivity. Unlike most previously studied platinum …
Aerobic C-C And C-O Bond Formation Reactions Mediated By High-Valent Nickel Species., Sofia Smith, Oriol Planas, Laura Gómez, Nigam Rath, Xavi Ribas, Liviu Mirica, Liviu Mirica
Aerobic C-C And C-O Bond Formation Reactions Mediated By High-Valent Nickel Species., Sofia Smith, Oriol Planas, Laura Gómez, Nigam Rath, Xavi Ribas, Liviu Mirica, Liviu Mirica
Chemistry & Biochemistry Faculty Works
Nickel complexes have been widely employed as catalysts in C–C and C–heteroatom bond formation reactions. While Ni(0), Ni(I), and Ni(II) intermediates are most relevant in these transformations, recently Ni(III) and Ni(IV) species have also been proposed to play a role in catalysis. Reported herein is the synthesis, detailed characterization, and reactivity of a series of Ni(II) and Ni(III) metallacycle complexes stabilized by tetradentate pyridinophane ligands with various N-substituents. Interestingly, while the oxidation of the Ni(II) complexes with various other oxidants led to exclusive C–C bond formation in very good yields, the use of O2 or H2O2 as oxidants led to …
Understanding Interactions Of Citropin 1.1 Analogues With Model Membranes And Their Influence On Biological Activity, Nathalia Rodrigues De Almeida, Jonathan Catazaro, Maddeboina Krishnaiah, Yashpal Singh Chhonker, Daryl J. Murry, Robert Powers, Martin Conda-Sheridan
Understanding Interactions Of Citropin 1.1 Analogues With Model Membranes And Their Influence On Biological Activity, Nathalia Rodrigues De Almeida, Jonathan Catazaro, Maddeboina Krishnaiah, Yashpal Singh Chhonker, Daryl J. Murry, Robert Powers, Martin Conda-Sheridan
Department of Chemistry: Faculty Publications
The rapid emergence of resistant bacterial strains has made the search for new antibacterial agents an endeavor of paramount importance. Cationic antimicrobial peptides (AMPs) have the ability to kill resistant pathogens while diminishing the development of resistance. Citropin 1.1 (Cit 1.1) is an AMP effective against a broad range of pathogens. 20 analogues of Cit 1.1 were prepared to understand how sequence variations lead to changes in structure and biological activity. Various analogues exhibited an increased antimicrobial activity relative to Cit 1.1. The two most promising, AMP-016 (W3F) and AMP-017 (W3F, D4R, K7R) presented a 2- to 8-fold increase in …
A Panel Of Protein Kinase Chemosensors Distinguishes Different Types Of Fatty Liver Disease, Jon R. Beck, Fatima Cabral, Karuna Rasineni, Carol A. Casey, Edward N. Harris, Cliff I. Stains
A Panel Of Protein Kinase Chemosensors Distinguishes Different Types Of Fatty Liver Disease, Jon R. Beck, Fatima Cabral, Karuna Rasineni, Carol A. Casey, Edward N. Harris, Cliff I. Stains
Department of Chemistry: Faculty Publications
The worldwide incidence of fatty liver disease continues to rise, which may account for concurrent increases in the frequencies of more aggressive liver ailments. Given the existence of histologically identical fatty liver disease subtypes, there is a critical need for the identification of methods that can classify disease and potentially predict progression. Herein, we show that a panel of protein kinase chemosensors can distinguish fatty liver disease subtypes. These direct activity measurements highlight distinct differences between histologically identical fatty liver diseases arising from diets rich in fat versus alcohol and identify a previously unreported decrease in p38α activity associated with …
Systematic Optimization For Production Of The Anti-Mrsa Antibiotics Wap-8294a In An Engineered Strain Of Lysobacter Enzymogenes, Xusheng Chen, Shanren Li, Lingjun Yu, Amanda Miller, Liangcheng Du
Systematic Optimization For Production Of The Anti-Mrsa Antibiotics Wap-8294a In An Engineered Strain Of Lysobacter Enzymogenes, Xusheng Chen, Shanren Li, Lingjun Yu, Amanda Miller, Liangcheng Du
Department of Chemistry: Faculty Publications
WAP-8294A is a group of cyclic lipodepsipeptides and considered as the first-in-class new chemical entity with potent activity against methicillin-resistant Staphylococcus aureus. One of the roadblocks in developing the WAP-8294A antibiotics is the very low yield in Lysobacter. Here, we carried out a systematic investigation of the nutritional and environmental conditions in an engineered L. enzymogenes strain for the optimal production of WAP-8294A. We developed an activity-based simple method for quick screening of various factors, which enabled us to optimize the culture conditions. With the method, we were able to improve the WAP-8294A yield by 10-fold in small-scale cultures and …
Development Of A Screening Method For Drugs Of Abuse By Direct Analysis Of Dried Urine Spots Coupled To Mass Spectrometry, Melanie Goldstein
Development Of A Screening Method For Drugs Of Abuse By Direct Analysis Of Dried Urine Spots Coupled To Mass Spectrometry, Melanie Goldstein
Student Theses
Fast and easy screening procedures are essential in any forensic toxicology laboratory to differentiate negative samples from presumptive positive cases. Immunoassay techniques, such as enzyme multiplied immunoassay technique (EMIT), are routinely employed as screening procedures. However, these techniques lack specificity (only differentiate group of drugs and not individual compounds) and it is difficult to add new compounds to the panel. Direct analysis of dried urine spots (DUS) by mass spectrometry (MS) offers a novel strategy to overcome these issues. DUS offer an improved storage alternative for biological samples, reducing costs and space requirements. In this work, an original method to …
The Effects Of Active Site And Allosteric Residues On Catalysis And Inhibitor Selectivity In The Bacillus Stearothennophilus Dihydrofolate Reductase, Tyler Eck
Theses, Dissertations and Culminating Projects
In drug discovery, building a comprehensive picture of the binding events between a drug and its enzyme target can be useful, especially in the development of new drugs or predicting the effect of a drug on a similar target from the same protein family. It is well known that a drug's selectivity is influenced by its interactions with amino acid residues within the active site, but contributions from residues situated away from (distal to) the active site are less well understood. Using a novel predictive approach PAnPredictor that employs sequence alignments, we have previously predicted residue positions in the dihydrofolate …
Development Of Ni-Catalyzed Alkene Dicarbofunctionalization Reactions, Shekhar Kc
Development Of Ni-Catalyzed Alkene Dicarbofunctionalization Reactions, Shekhar Kc
Chemistry and Chemical Biology ETDs
Alkenes serve as one of the most important feedstocks for organic synthesis, having two vicinal sites for bond formation. In alkenes, both vicinal sites can be functionalized with two reagents in a process commonly known as alkene difunctionalization, which results in the formation of two new bonds. A number of alkenes difunctionalization reactions, such as diamination, dioxygenation, carboamination and carbooxygenation, are known. However, difunctionalization of alkenes with two carbon-based entities, termed alkene dicarbofunctionalization, is relatively less common. Development of such a process could provide a powerful method to introduce two different carbon fragments across an alkene in a regioselective manner, …
Optimization Of Protein Entrapment In Affinity Microcolumns Using Hydrazide-Activated Silica And Glycogen As A Capping Agent, John Vargas-Badilla, Saumen Poddar, Shiden Azaria, Chenhua Zhang, David S. Hage
Optimization Of Protein Entrapment In Affinity Microcolumns Using Hydrazide-Activated Silica And Glycogen As A Capping Agent, John Vargas-Badilla, Saumen Poddar, Shiden Azaria, Chenhua Zhang, David S. Hage
David Hage Publications
Several approaches were compared for the entrapment of proteins within hydrazide-activated silica for use in affinity microcolumns and high performance affinity chromatography. Human serum albumin (HSA) and concanavalin A (Con A) were used as model proteins for this work. Items considered in this study included the role played by the solution volume, amount of added protein, and use of slurry vs. on-column entrapment on the levels of solute retention and extent of protein immobilization that could be obtained by means of entrapment. The levels of retention and protein immobilization were evaluated by injecting warfarin or 4-methylumbellipheryl α-D-mannopyranoside as solutes with …
Investigating Color Additive Molecules For Pharmaceutical And Cosmetic Applications: A Comparison Of Theoretical And Experimental Uv-Visible Absorbance Spectra In Tunable Solvents, Jacqueline Casey Mohen
Investigating Color Additive Molecules For Pharmaceutical And Cosmetic Applications: A Comparison Of Theoretical And Experimental Uv-Visible Absorbance Spectra In Tunable Solvents, Jacqueline Casey Mohen
Theses and Dissertations
Color additive molecules have widespread applications ranging from ingestible foods and pharmaceutics to non-ingestible cosmetics and other naturally or synthetically developed consumer products available worldwide. Certification for approved use of color additives varies globally; therefore, a feasible method to analyze existing color additives or to design novel color additive molecules with enhanced or otherwise desired physicochemical properties (such as hue) is in high demand for universal adoption. The studies herein provide sufficient proof that density functional theory and time-dependent density functional theory serve as effective predictive modeling techniques for generating theoretical maximum absorbance spectral peak responsivity for a single color …
Integration Of Random Forest Classifiers And Deep Convolutional Neural Networks For Classification And Biomolecular Modeling Of Cancer Driver Mutations, Steve Agajanian, Odeyemi Oluyemi, Gennady M. Verkhivker
Integration Of Random Forest Classifiers And Deep Convolutional Neural Networks For Classification And Biomolecular Modeling Of Cancer Driver Mutations, Steve Agajanian, Odeyemi Oluyemi, Gennady M. Verkhivker
Mathematics, Physics, and Computer Science Faculty Articles and Research
Development of machine learning solutions for prediction of functional and clinical significance of cancer driver genes and mutations are paramount in modern biomedical research and have gained a significant momentum in a recent decade. In this work, we integrate different machine learning approaches, including tree based methods, random forest and gradient boosted tree (GBT) classifiers along with deep convolutional neural networks (CNN) for prediction of cancer driver mutations in the genomic datasets. The feasibility of CNN in using raw nucleotide sequences for classification of cancer driver mutations was initially explored by employing label encoding, one hot encoding, and embedding to …
Determination Of Anxiolytic And Antidepressant Medicines In New York City Wastewater Samples, Jasmine J. Gayle
Determination Of Anxiolytic And Antidepressant Medicines In New York City Wastewater Samples, Jasmine J. Gayle
Student Theses
Wastewater-based epidemiology (WBE) provides information about a population’s exposure to certain chemical agents, such as drugs of abuse and medicines, by the analysis of human biomarkers, also known as excretion products, in wastewater samples. Although this is a growing field worldwide, mainly in Europe, Oceania, and Asia, limited data from the US are currently available. We developed and validated an analytical method to quantitatively and qualitatively determine the presence of commonly prescribed drugs to treat anxiety (alprazolam, buspirone, clonazepam, lorazepam, and propranolol) and depression (bupropion, citalopram, clomipramine, duloxetine, fluoxetine, imipramine, paroxetine, sertraline, and venlafaxine) in wastewater using liquid chromatography tandem …
Investigations Of The Mechanism Of Action For Lung Cancer Cell Death By A 4-Trifluoromethoxy Substituted Chalcone, Trevor M. Stantliff
Investigations Of The Mechanism Of Action For Lung Cancer Cell Death By A 4-Trifluoromethoxy Substituted Chalcone, Trevor M. Stantliff
Undergraduate Theses
Chalcones are a diphenyl compound that serves as a natural precursor to flavonoids in plants. Chalcones have been shown to have anticancer and antimicrobial activities. Chemoprevention activity of chalcones are of high interest in medicinal chemistry because of the simple laboratory synthesis and modification via Claisen-Schmidt condensation. Previously this lab created and screened a library of synthetic chalcones against A549 lung adenocarcinoma cell line for antiproliferation properties. We identified a strong drug candidate (4-trifluoromethoxy substituted chalcone) for A549 growth inhibition. However, the cause of inhibition by the substituted chalcone remains to be identified We began to explore the mechanism of …
Manipulation Of Noncovalent Interactions For The Synthesis And Use Of Natural Product Synthons, Alison P. Hart
Manipulation Of Noncovalent Interactions For The Synthesis And Use Of Natural Product Synthons, Alison P. Hart
Dissertations
Natural products are widely used in the pharmaceutical industry, in agriculture, and as specialty chemicals. Methodology development focuses on optimizing the key organic reactions to access these natural products while trying to limit the overall number of synthetic steps. Key bond forming strategies are sought to provide new ways to address carbon-carbon or carbon-heteroatom bonds. The advancement of new asymmetric reactions to generate enantiopure products from achiral starting materials is a vital area of research. The objectives addressed in this dissertation include: 1) the development of a general reductive conversion of esters to ethers with a broad substrate scope accessing …
The Characterization Of A New Metabolite From A Trichodesmium Bloom, Kelly M. Mcmanus
The Characterization Of A New Metabolite From A Trichodesmium Bloom, Kelly M. Mcmanus
Senior Honors Projects
Our laboratory has been investigating blooms of Trichodesmium, a genus of ecologically important, nitrogen-fixing cyanobacteria, collected from Padre Island in the Gulf of Mexico. Trichodesmium species are an underexplored biological source of cyanobacteria – a taxa that has been shown to produce chemically diverse secondary metabolites. With our focus on the isolation and structure characterization of new bioactive marine natural products, our research group has discovered over 25 new-to-science compounds over the past three years from these blooms. UV and mass spectrometry-guided isolation of Trichodesmium chromatography fractions were utilized to isolate a new metabolite. Isolation of this metabolite was …
The Use Of Heterocycles As Important Structures In Medicinal Chemistry, Sayre Weast
The Use Of Heterocycles As Important Structures In Medicinal Chemistry, Sayre Weast
Honors Theses
Heterocycles have many applications in the discipline of medicinal chemistry. These structures are found in various natural products with relevant biological activity. Our research group, in collaboration with two others, is particularly interested in one heterocycle, quinoline, as a scaffold for HIV-1 integrase inhibitors. A synthetic route has been developed to produce a derivatized structure on small scale. One goal of this thesis was to expand the scale of this route to provide increased quantities of the quinoline scaffold. Procedures were adapted to accommodate the increase in scale to convert commercially available anthranilic acids to quinolines via the isatoic anhydride. …
Preparation Of Enantioenriched Alkyltin Species And Their Application In Stereospecific Transformations, Glenn O. Ralph
Preparation Of Enantioenriched Alkyltin Species And Their Application In Stereospecific Transformations, Glenn O. Ralph
Dissertations, Theses, and Capstone Projects
Organometallic reagents containing the tin-carbon bond are used extensively in modern synthetic chemistry for the formation of new bonds to carbon. Over recent decades, transition metal catalyzed cross coupling reactions between two C(sp2) centers have been widely developed. However, the introduction of a C(sp3) center complicates the catalytic cycle, and opens unproductive chemical pathways which lead to isomerization, elimination, and racemization. Our lab has developed a modified-Stille reaction to combat the deleterious effects of β-hydride elimination. Our protocol enables unactivated 2° alkyl organotin nucleophiles to undergo efficient cross coupling reactions with C(sp2) electrophiles, avoiding …
A Pretargeted Spect Imaging Strategy Employing Technetium-99m Based On Bioorthogonal Diels-Alder Click Chemistry, Justin H. Walsh
A Pretargeted Spect Imaging Strategy Employing Technetium-99m Based On Bioorthogonal Diels-Alder Click Chemistry, Justin H. Walsh
Dissertations, Theses, and Capstone Projects
A series of related N3S 99mTc-peptide complexes were synthesized and tested for use in pretargeting SPECT imaging that utilizes the bioorthogonal Diels-Alder click reaction between tetrazine (Tz) and transcyclooctene (TCO). The objective was to optimize the excretory pathways of the 99mTc-peptide complexes for maximum tumor targeting with the in vivo “click” and minimum non-target uptake. The 99mTc–tetrazine constructs were prepared by reaction of 99mTc-peptide complexes (99mTc-FKC, 99mTc-FKCR, 99mTc-DKC, and 99mTc-SKC) with Tz-NHS or Tz-PEG5-NHS to form 99mTc FK(Tz)C, 99mTc-FK(PEG5-Tz)CR, 99mTc-DK(PEG5-Tz)C, …
Coumarins And P450s, Studies Reported To-Date, Maryam Foroozesh, Jayalakshmi Sridhar, Navneet Goyal, Jiawang Liu
Coumarins And P450s, Studies Reported To-Date, Maryam Foroozesh, Jayalakshmi Sridhar, Navneet Goyal, Jiawang Liu
Faculty and Staff Publications
Cytochrome P450 enzymes (CYPs) are important phase I enzymes involved in themetabolism of endogenous and xenobiotic compounds mainly through mono-oxygenation reactions into more polar and easier to excrete species. In addition to their role in detoxification, they play important roles in the biosynthesis of endogenous compounds and the bioactivation of xenobiotics. Coumarins, phytochemicals abundant in food and commonly used in fragrances and cosmetics, have been shown to interact with P450 enzymes as substrates and/or inhibitors. In this review, these interactions and their significance in pharmacology and toxicology are discussed in detail.
Mechanistic Studies And Derivative Effects In 1, 3, 4- Oxadiazole Synthesis Via Cyclodehydration Reactions, Evan Huggins
Mechanistic Studies And Derivative Effects In 1, 3, 4- Oxadiazole Synthesis Via Cyclodehydration Reactions, Evan Huggins
Undergraduate Honors Thesis Projects
In the world of pharmaceutical synthesis, research to combat foreign pathogens is always necessary. Scientists have been exploring different methods in order to synthesize the most effective compounds in antibacterial, anticancer, anti-inflammatory, and many other treatments. A key component within these versatile compounds are 1,3,4-oxadiazoles. Current methods to synthesize these compounds are inefficient. This research seeks to improve oxadiazole synthesis; however, the mechanism of this reaction is unknown. The goal of this project was to study the mechanistic pathway in the discovered, one-pot cyclodehydration synthesis of 1,3,4-oxadiazoles. In the first part of this study, a diacylhydrazine intermediate was proposed. This …
The Effects Of Cannabidiol And Delta 9-Tetrahydrocannabinol Concentration On Breast Cancer Cells, Dorothy Agyemang
The Effects Of Cannabidiol And Delta 9-Tetrahydrocannabinol Concentration On Breast Cancer Cells, Dorothy Agyemang
Ursidae: The Undergraduate Research Journal at the University of Northern Colorado
Delta 9-tetrahydrocannabinol (THC) and cannabidiol (CBD) are phytocannabinoids that have a potential impact on cancer treatments. Studies have shown that certain cannabinoids cause cancer cells to die, but only with the right concentration, which has not been well documented. The purpose of this study is to determine the exact concentration of CBD and THC needed to kill MCF-7 breast cancer cells. In this experiment, the initial treatment group will be treated with CBD or THC at concentrations of 0.1, 1, 10 and 100 micromolar. These concentrations were arbitrarily chosen because there is not an established baseline. Cell metabolic activity will …
Development Of Ruthenium Drugs As Anticancer Agents, Daniel Boy
Development Of Ruthenium Drugs As Anticancer Agents, Daniel Boy
Chemistry & Biochemistry Student Projects
An overview of literature that outlines the research methods of the development of proposed Ruthenium based anti-cancer agents.
A Quantitative Lc-Ms/Ms Method For Determination Of A Small Molecule Agonist Of Epha2 In Mouse Plasma And Brain Tissue, Bo Zhong, Yaxin Li, Nethrie Idippily, Aaron Petty, Bin Su Ph.D., Bingcheng Wang
A Quantitative Lc-Ms/Ms Method For Determination Of A Small Molecule Agonist Of Epha2 In Mouse Plasma And Brain Tissue, Bo Zhong, Yaxin Li, Nethrie Idippily, Aaron Petty, Bin Su Ph.D., Bingcheng Wang
Chemistry Faculty Publications
Compound 27 {1, 12‐bis[4‐(4‐amino‐6,7‐dimethoxyquinazolin‐2‐yl)piperazin‐1‐yl]dodecane‐1,12‐dione} is a novel small molecule agonist of EphA2 receptor tyrosine kinase. It showed much improved activity for the activation of EphA2 receptor compared with the parental compound doxazosin. To support further pharmacological and toxicological studies of the compound, a method using liquid chromatography and electrospray ionization tandem mass spectrometry (LC–MS/MS) has been developed for the quantification of this compound. Liquid–liquid extraction was used to extract the compound from mouse plasma and brain tissue homogenate. Reverse‐phase chromatography with gradient elution was performed to separate compound 27 from the endogenous molecules in the matrix, followed by …
Analysis Of Drug–Protein Interactions During Diabetes By High-Performance Affinity Chromatography, Pingyang Tao
Analysis Of Drug–Protein Interactions During Diabetes By High-Performance Affinity Chromatography, Pingyang Tao
Department of Chemistry: Dissertations, Theses, and Student Research
High-performance affinity chromatography (HPAC) is a type of liquid chromatography in which solutes are separated based on their binding to a stationary phase that is a biologically-related agent. Sulfonylurea drugs have significant binding to proteins in blood, with most of this binding is believed to occur with human serum albumin (HSA). HSA is known to be modified as a result of the high serum levels of glucose that is present during diabetes, which may also alter the function of HSA as a binding agent for many drugs in circulation. Some modifications of HSA that can occur during diabetes involves early …
An Improved Synthesis Of Adefovir And Related Analogues, Timothy P. O'Sullivan, Et Al
An Improved Synthesis Of Adefovir And Related Analogues, Timothy P. O'Sullivan, Et Al
Physical Sciences Publications
An improved synthesis of the antiviral drug adefovir is presented. Problems associated with current routes to adefovir include capricious yields and a reliance on problematic reagents and solvents, such as magnesium tert-butoxide and DMF, to achieve high conversions to the target. A systematic study within our laboratory led to the identification of an iodide reagent which affords higher yields than previous approaches and allows for reactions to be conducted up to 10 g in scale under milder conditions. The use of a novel tetrabutylammonium salt of adenine facilitates alkylations in solvents other than DMF. Additionally, we have investigated how …
Lew.1wr1 Rats Have Altered Inflammation Responses During Type 1 Diabetes Induction, Madushika Wimalarathne, Kayleigh Cantrell, Joshua Derbort
Lew.1wr1 Rats Have Altered Inflammation Responses During Type 1 Diabetes Induction, Madushika Wimalarathne, Kayleigh Cantrell, Joshua Derbort
Research Horizons Day Posters
No abstract provided.
Tracking Decitabine Incorporation Into Malignant Myeloid Cell Dna In Vitro And In Vivo By Lc-Ms/Ms With Enzymatic Digestion, Sujatha Chilakala, Ye Feng, Lan Li, Reda Mahfouz, Ebrahem Quteba, Yogen Saunthararajah, Yan Xu
Tracking Decitabine Incorporation Into Malignant Myeloid Cell Dna In Vitro And In Vivo By Lc-Ms/Ms With Enzymatic Digestion, Sujatha Chilakala, Ye Feng, Lan Li, Reda Mahfouz, Ebrahem Quteba, Yogen Saunthararajah, Yan Xu
Chemistry Faculty Publications
The DNA hypomethylating agents decitabine and 5-azacytidine are the only two drugs approved for treatment of all subtypes of the myeloid malignancy myelodysplastic syndromes (MDS). The key to drug activity is incorporation into target cell DNA, however, a practical method to measure this incorporation is un-available. Here, we report a sensitive and specific LC-MS/MS method to simultaneously measure decitabine incorporation and DNA hypomethylation. A stable heavy isotope of 2'-deoxycytidine was used as an internal standard and one-step multi-enzyme digestion was used to release the DNA bound drug. Enzyme-released decitabine along with other mononucleosides were separated by a reverse-phase C-18 column …
Purification And Characterization Of A Nonspecific Lipid Transfer Protein 1 (Nsltp1) From Ajwain (Trachyspermum Ammi) Seeds, Meshal Nazeer, Humera Waheed, Maria Saeed, Saman Yousuf Ali, M. Iqbal Choudhary, Zaheer Ul-Haq, Aftab Ahmed
Purification And Characterization Of A Nonspecific Lipid Transfer Protein 1 (Nsltp1) From Ajwain (Trachyspermum Ammi) Seeds, Meshal Nazeer, Humera Waheed, Maria Saeed, Saman Yousuf Ali, M. Iqbal Choudhary, Zaheer Ul-Haq, Aftab Ahmed
Pharmacy Faculty Articles and Research
Ajwain (Trachyspermum ammi) belongs to the family Umbelliferae, is commonly used in traditional, and folk medicine due to its carminative, stimulant, antiseptic, diuretic, antihypertensive, and hepatoprotective activities. Non-specific lipid transfer proteins (nsLTPs) reported from various plants are known to be involved in transferring lipids between membranes and in plants defense response. Here, we describe the complete primary structure of a monomeric non-specific lipid transfer protein 1 (nsLTP1), with molecular weight of 9.66 kDa, from ajwain seeds. The nsLTP1 has been purified by combination of chromatographic techniques, and further characterized by mass spectrometry, and Edman degradation. The ajwain nsLTP1 …
Synthesis Of A Sulfur Variant For Treatment Of Trypanosomiasis, Carlos Vera-Esquivel
Synthesis Of A Sulfur Variant For Treatment Of Trypanosomiasis, Carlos Vera-Esquivel
UNO 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)) …
Synthesis, Biological Evaluation And Molecular Modeling Studies Of Novel Chromone/Aza-Chromone Fused Α-Aminophosphonates As Src Kinase Inhibitors, S. Bapat, N. Viswanadh, M. Mujahid, Amir Nasrolahi Shirazi, Rakesh Tiwari, Keykavous Parang, M. Karthikeyan, M. Muthukrishnan, Renu Vyas
Synthesis, Biological Evaluation And Molecular Modeling Studies Of Novel Chromone/Aza-Chromone Fused Α-Aminophosphonates As Src Kinase Inhibitors, S. Bapat, N. Viswanadh, M. Mujahid, Amir Nasrolahi Shirazi, Rakesh Tiwari, Keykavous Parang, M. Karthikeyan, M. Muthukrishnan, Renu Vyas
Pharmacy Faculty Articles and Research
A series of novel chromone/aza-chromone fused α-aminophosphonate derivatives were synthesized in good yields using silica chloride as the catalyst. All the synthesized compounds were tested for their c-Src kinase inhibitory activity. Aza-chromone compound showed Src kinase inhibition with an IC50 value of 15.8 µM. The compounds were subjected to molecular docking and dynamics simulations to study the atomic level interactions with an unphosphorylated proto-oncogenic tyrosine protein kinase Src (PDB code 1Y57) as well as phosphorylated tyrosine protein kinase Src (PDB code 2H8H). Docking and molecular dynamic results revealed phosphorylated Src tyrosine kinase protein better results than unphosphorylated tyrosine Src kinase …