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Articles 181 - 210 of 397

Full-Text Articles in Chemistry

Development Of Lc-Ms/Ms Methods For Quantitative Analysis Of Plant-Derived Anticancer Agent And Synthetic Estrogen In Complex Matrices, Simuli Lindah Wabuyele Jan 2013

Development Of Lc-Ms/Ms Methods For Quantitative Analysis Of Plant-Derived Anticancer Agent And Synthetic Estrogen In Complex Matrices, Simuli Lindah Wabuyele

ETD Archive

No abstract provided.


Automated Spectral Identification Of Materials Using Spectral Identity Mapping, Robert William Cannon Jan 2013

Automated Spectral Identification Of Materials Using Spectral Identity Mapping, Robert William Cannon

ETD Archive

With increased use of Raman spectroscopic instrumentation for material analysis there has also been an increase in the amount of acquired Raman spectral data. Because of this, there is a clear need to develop and implement advanced spectral analysis techniques. This is especially true in cases where limited reference data may be available and large data sets need to be interpreted. Raman spectral analysis and standardization techniques, along with a foundation for a comprehensive repository of Raman spectral data, will be described in this thesis. The main focus will be automated analysis and standardization of Raman spectral data using spectral …


Nos Oxygenase-Mediated Nitroalkane Catalytic Reduction: Impact On Nos Reaction, Praneeth Ivan Joel Fnu Jan 2013

Nos Oxygenase-Mediated Nitroalkane Catalytic Reduction: Impact On Nos Reaction, Praneeth Ivan Joel Fnu

ETD Archive

Organic nitroalkanes are used in many industries and for a variety of purposes. Their use is expanding and is steadily claiming new territories in our immediate environment. Some nitroalkanes, when they enter the human body, can be harmful as such or can be activated to generate reactive intermediates with known detrimental effects. P450 enzymes are known for metabolizing a variety of drugs and substances including organic nitroalkanes. Nitric oxide synthases (NOS) exhibit some similarities to P450 metalloenzymes and their potential interaction with nitroalkanes as xenobiotics is not well known. The present study investigates the effect of nitroalkanes on the catalytic …


Synthesis And Evaluation Of Some 17-Acetamidoandrostane And N,N-Dimethyl-7-Deoxycholic Amide Derivatives As Cytotoxic Agents: Structure/Activity Studies, Yanmin Huang, Jianguo Cui, Linyi Jia, Chunfang Gan, Huacan Song, Chun Zeng, Aimin Zhou Jan 2013

Synthesis And Evaluation Of Some 17-Acetamidoandrostane And N,N-Dimethyl-7-Deoxycholic Amide Derivatives As Cytotoxic Agents: Structure/Activity Studies, Yanmin Huang, Jianguo Cui, Linyi Jia, Chunfang Gan, Huacan Song, Chun Zeng, Aimin Zhou

Chemistry Faculty Publications

Using pregnenolone and 7-deoxycholic acid as starting materials, some 17-acetamidoandrostane and N,N-dimethyl-7-deoxycholic amide derivatives were synthesized. The cytotoxicity of the synthesized compounds was tested in vitro against two tumor cell lines: SGC 7901 (human gastric carcinoma) and Bel 7404 (human liver carcinoma). The result showed that the blockage of the interaction of the amide group with outside groups might cause a decrease of the cytotoxicity, and an O-benzyloximino group at the 3-position of N,N-dimethyl-7-deoxycholic amide could enhance the cytotoxic activity of the compound. The information obtained from the studies provides the structure-activity relationship for these compounds and may be useful …


Charge-Pairing Interactions Control The Conformational Setpoint And Motions Of The Fmn Domain In Neuronal Nitric Oxide Synthase, Mohammad Mahfuzul Haque, Mekki Bayachou, Mohammed A. Fadlalla, Deborah Durra, Dennis J. Stuehr Jan 2013

Charge-Pairing Interactions Control The Conformational Setpoint And Motions Of The Fmn Domain In Neuronal Nitric Oxide Synthase, Mohammad Mahfuzul Haque, Mekki Bayachou, Mohammed A. Fadlalla, Deborah Durra, Dennis J. Stuehr

Chemistry Faculty Publications

The NOS (nitric oxide synthase; EC 1.14.13.39) enzymes contain a C-terminal flavoprotein domain [NOSred (reductase domain of NOS)] that binds FAD and FMN, and an N-terminal oxygenase domain that binds haem. Evidence suggests that the FMN-binding domain undergoes large conformational motions to shuttle electrons between the NADPH/FAD-binding domain [FNR (ferredoxin NADP-reductase)] and the oxygenase domain. Previously we have shown that three residues on the FMN domain (Glu(762), Glu(816) and Glu(819)) that make charge-pairing interactions with the FNR help to slow electron flux through nNOSred (neuronal NOSred). In the present study, we show that charge neutralization or reversal at each of …


Voltage-Controlled Enzyme-Catalyzed Glucose–Gluconolactone Conversion Using A Field-Effect Enzymatic Detector, Siu Tung Yau, Yan Xu, Yang Song, Ye Feng, Jiapeng Wang Jan 2013

Voltage-Controlled Enzyme-Catalyzed Glucose–Gluconolactone Conversion Using A Field-Effect Enzymatic Detector, Siu Tung Yau, Yan Xu, Yang Song, Ye Feng, Jiapeng Wang

Chemistry Faculty Publications

The field-effect enzymatic detection (FEED) technique was used to control the kinetics of the enzymatic conversion of glucose to gluconolactone. The glucose–gluconolactone conversion occurring at an enzyme-immobilized electrode, a well-studied process, was confirmed using mass spectrometry. Electrochemical studies showed that the glucose oxidation current depends on the gating voltage VG and the ion concentration of the sample solution. Additionally, the depletion of glucose in the sample also showed a dependence on VG. FEED was used to detect H2O2 on the zepto-molar level in order to show the ultrasensitive detection capability of the technique. These results, while providing evidence for the …


Spectroscopic Analysis Of Polymerization And Exonuclease Proofreading By A High-Fidelity Dna Polymerase During Translesion Dna Synthesis, Babho Devadoss, Irene Lee, Anthony J. Berdis Jan 2013

Spectroscopic Analysis Of Polymerization And Exonuclease Proofreading By A High-Fidelity Dna Polymerase During Translesion Dna Synthesis, Babho Devadoss, Irene Lee, Anthony J. Berdis

Chemistry Faculty Publications

High fidelity DNA polymerases maintain genomic fidelity through a series of kinetic steps that include nucleotide binding, conformational changes, phosphoryl transfer, polymerase translocation, and nucleotide excision. Developing a comprehensive understanding of how these steps are coordinated during correct and pro-mutagenic DNA synthesis has been hindered due to lack of spectroscopic nucleotides that function as efficient polymerase substrates. This report describes the application of a non-natural nucleotide designated 5-naphthyl-indole-2′-deoxyribose triphosphate which behaves as a fluorogenic substrate to monitor nucleotide incorporation and excision during the replication of normal DNA versus two distinct DNA lesions (cyclobutane thymine dimer and an abasic site). Transient …


The Association Of Elevated 2′,5′-Oligoadenylate-Dependent Rnase L With Lung Cancer Correlated With Deficient Enzymatic Activity And Decreased Capacity Of Rnase L Dimerization, Huijing Yin, Aimin Zhou, Yalei Dai Oct 2012

The Association Of Elevated 2′,5′-Oligoadenylate-Dependent Rnase L With Lung Cancer Correlated With Deficient Enzymatic Activity And Decreased Capacity Of Rnase L Dimerization, Huijing Yin, Aimin Zhou, Yalei Dai

Chemistry Faculty Publications

RNase L mediates critical cellular functions including antiviral, proapoptotic, antiproliferative and tumor suppressive activities. In this study, the expression and function of RNase L in lung cancer cells were examined. Interestingly we have found that the expression of RNase L in lung cancer cells was 3- and 9-fold higher in its mRNA and protein levels, but a significant decrease of its enzymatic activity when compared to that in corresponding normal lung cells. Further investigation revealed that 2-5A-induced dimerization of the RNase L protein, a necessary prerequisite for activation of RNase L, was inhibited, as a result of that RLI, a …


Cox Inhibitors Indomethacin And Sulindac Derivatives As Antiproliferative Agents: Synthesis, Biological Evaluation, And Mechanism Investigation, Snigdha Chennamaneni, Bo Zhong, Rati Lama, Bin Su Oct 2012

Cox Inhibitors Indomethacin And Sulindac Derivatives As Antiproliferative Agents: Synthesis, Biological Evaluation, And Mechanism Investigation, Snigdha Chennamaneni, Bo Zhong, Rati Lama, Bin Su

Chemistry Faculty Publications

Cyclooxygenase (COX) inhibitors Indomethacin and its structural analogs Sulindac exhibit cell growth inhibition and apoptosis inducing activities in various cancer cell lines via COX independent mechanisms. In this study, the molecular structures of Indomethacin and Sulindac were used as starting scaffolds to design novel analogs and their effects on the proliferation of human cancer cells were evaluated. Compared to Indomethacin and Sulindac inhibiting cancer cell proliferation with IC50s of more than 1 mM, the derivatives displayed significantly increased activities. Especially, one of the Indomethacin analogs inhibited the growth of a series of cancer cell lines with IC50s around 0.5 μM–3 …


Exploring The Role Of A Conserved Class A Residue In The Ω-Loop Of Kpc-2 Β-Lactamase: A Mechanism For Ceftazidime Hydrolysis Sep 2012

Exploring The Role Of A Conserved Class A Residue In The Ω-Loop Of Kpc-2 Β-Lactamase: A Mechanism For Ceftazidime Hydrolysis

Chemistry Faculty Publications

Gram-negative bacteria harboring KPC-2, a class A β-lactamase, are resistant to all β-lactam antibiotics and pose a major public health threat. Arg-164 is a conserved residue in all class A β-lactamases and is located in the solvent-exposed Ω-loop of KPC-2. To probe the role of this amino acid in KPC-2, we performed site-saturation mutagenesis. When compared with wild type, 11 of 19 variants at position Arg-164 in KPC-2 conferred increased resistance to the oxyimino-cephalosporin, ceftazidime (minimum inhibitory concentration; 32→128 mg/liter) when expressed in Escherichia coli. Using the R164S variant of KPC-2 as a representative β-lactamase for more detailed analysis, we …


Synthesis And Characterization Of Chain-End Functionalization Of Glycosaminoglycans, Nikola Paulic, Jacob J. Weingart Sep 2012

Synthesis And Characterization Of Chain-End Functionalization Of Glycosaminoglycans, Nikola Paulic, Jacob J. Weingart

Undergraduate Research Posters 2012

This presentation reports the CSU Summer Undergraduate Research project, which is the synthesis and characterization of chain-end functionalized CS derivatives, which will be used to investigate various bio-orthogonal conjugation reactions in attempt to create a novel CS-rTM conjugate.


Differential Protein Expression In Polystichum Acrostichoides Due To Metal Exposure, Paul Alexander Ilkanich, Pratheek C. Koneru Sep 2012

Differential Protein Expression In Polystichum Acrostichoides Due To Metal Exposure, Paul Alexander Ilkanich, Pratheek C. Koneru

Undergraduate Research Posters 2012

Plants are considered the most cost effective and environmentally sound way to clean up the soils and water contaminated with toxic metals. We focused our studies on the fern species Polystichum acrostichoides. A total of 17 protein spots were up regulated and 3 proteins were down regulated upon various metal exposures, and are arranged to be subjected to liquid chromatography-tandem mass spectrometry for further identification.


Derivatization Of Free Glycans For Glycan Sensor And Glyco-Functionalization Applications, Rhonda D. Jones Sep 2012

Derivatization Of Free Glycans For Glycan Sensor And Glyco-Functionalization Applications, Rhonda D. Jones

Undergraduate Research Posters 2012

Glycans, especially, cell surface glycans acting as receptors, are involved in a wide range of biological processes. Analysis of the cell surface glycans provides a basis for understanding the molecular mechanism of glycan-mediated biological process. The present method can be applied in derivatizing sugars from natural sources for glycan sensor and glyco-functionalization applications.


Rnase L Controls Terminal Adipocyte Differentiation, Lipids Storage And Insulin Sensitivity Via Chop10 Mrna Regulation, O. Fabre, T. Salehzada, K. Lambert, Y. Boo Seok, Aimin Zhou, J. Mercier, C. Bisbal Sep 2012

Rnase L Controls Terminal Adipocyte Differentiation, Lipids Storage And Insulin Sensitivity Via Chop10 Mrna Regulation, O. Fabre, T. Salehzada, K. Lambert, Y. Boo Seok, Aimin Zhou, J. Mercier, C. Bisbal

Chemistry Faculty Publications

Adipose tissue structure is altered during obesity, leading to deregulation of whole-body metabolism. Its function depends on its structure, in particular adipocytes number and differentiation stage. To better understand the mechanisms regulating adipogenesis, we have investigated the role of an endoribonuclease, endoribonuclease L (RNase L), using wild-type and RNase L-knockout mouse embryonic fibroblasts (RNase L−/−-MEFs). Here, we identify C/EBP homologous protein 10 (CHOP10), a dominant negative member of the CCAAT/enhancer-binding protein family, as a specific RNase L target. We show that RNase L is associated with CHOP10 mRNA and regulates its stability. CHOP10 expression is conserved in RNase …


Development And Validation Of A Rapid Lc-Ms/Ms Method Fortthe Determination Of Jcc76, A Novel Antitumor Agent For Breast Cancer, In Rat Plasma And Its Application To A Pharmacokinetics Study, Xiaohan Cai, Bo Zhong, Bin Su, Songlin Xu, Baochuan Guo Sep 2012

Development And Validation Of A Rapid Lc-Ms/Ms Method Fortthe Determination Of Jcc76, A Novel Antitumor Agent For Breast Cancer, In Rat Plasma And Its Application To A Pharmacokinetics Study, Xiaohan Cai, Bo Zhong, Bin Su, Songlin Xu, Baochuan Guo

Chemistry Faculty Publications

JCC76 is a novel nimesulide analog that selectively inhibits the human epidermal growth factor receptor 2 (HER2) overexpressing breast cancer cell proliferation and tumor progression. To support further pharmacological and toxicological studies of JCC76, a novel and rapid method using liquid chromatography and electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS) has been developed and validated for the quantification of the compound in rat plasma. A C18 column was used for chromatographic separation, and the mobile phase was aqueous ammonium formate (pH 3.7; 5 mm)–methanol (1:9, v/v) with an isocratic elution. With a simple liquid–liquid extraction procedure using the mixture of methyl …


Identification Of Selective Tubulin Inhibitors As Potential Anti-Trypanosomal Agents, Rati Lama, Ranjodh Sandhu, Bo Zhong, Bibo Li, Bin Su Sep 2012

Identification Of Selective Tubulin Inhibitors As Potential Anti-Trypanosomal Agents, Rati Lama, Ranjodh Sandhu, Bo Zhong, Bibo Li, Bin Su

Chemistry Faculty Publications

The potency of a series of sulfonamide tubulin inhibitors against the growth of Trypanosoma brucei (T. brucei), as well as human cancer and primary fibroblast cells were evaluated with the aim of determining whether compounds that selectively inhibit parasite proliferation could be identified. Several compounds showed excellent selectivity against T. brucei growth, and have the potential to be used for the treatment of Human African trypanosomiasis. A T. brucei tubulin protein homology model was built based on the crystal structure of the bovine tubulin. The colchicine-binding domain, which is also the binding site of the tested sulfonamide tubulin inhibitors, showed …


Understanding The Molecular Determinants Of Substrate And Inhibitor Specificities In The Carbapenemase Kpc-2: Exploring The Roles Of Arg220 And Glu276 Aug 2012

Understanding The Molecular Determinants Of Substrate And Inhibitor Specificities In The Carbapenemase Kpc-2: Exploring The Roles Of Arg220 And Glu276

Chemistry Faculty Publications

β-Lactamases are important antibiotic resistance determinants expressed by bacteria. By studying the mechanistic properties of β-lactamases, we can identify opportunities to circumvent resistance through the design of novel inhibitors. Comparative amino acid sequence analysis of class A β-lactamases reveals that many enzymes possess a localized positively charged residue (e.g., R220, R244, or R276) that is critical for interactions with β-lactams and β-lactamase inhibitors. To better understand the contribution of these residues to the catalytic process, we explored the roles of R220 and E276 in KPC-2, a class A β-lactamase that inactivates carbapenems and β-lactamase inhibitors. Our study reveals that substitutions …


Development And Validation Of An Lc–Ms/Ms Method For Pharmacokinetic Study Of Methoxyamine In Phase I Clinical Trial, Shuming Yang, Panayiotis Savvides, Lili Liu, Stanton L. Gerson, Yan Xu Jul 2012

Development And Validation Of An Lc–Ms/Ms Method For Pharmacokinetic Study Of Methoxyamine In Phase I Clinical Trial, Shuming Yang, Panayiotis Savvides, Lili Liu, Stanton L. Gerson, Yan Xu

Chemistry Faculty Publications

Methoxyamine (MX) is the first DNA base-excision-repair (BER) inhibitor evaluated in humans. This work described the development and validation of an LC–MS/MS method for quantitative determination of MX in human plasma. In this method, MX and its stable isotope methoxyl-d3-amine (MX-d3 as internal standard) were directly derivatized in human plasma with 4-(N,N-diethylamino)benzaldehyde. The derivatized MX and IS were extracted by methyl-tert-butyl ether, and separated isocratically on a Xterra C18 column (2.1 mm × 100 mm) using an aqueous mobile phase containing 45% acetonitrile and 0.4% formic acid at a flow rate of 0.200 ml/min. Quantitation of MX was carried out …


6-Hydroximino-4-Aza-A-Homo-Cholest-3-One And Related Analogue As A Potent Inducer Of Apoptosis In Cancer Cells, Yanmin Huang, Jianguo Cui, Qiaoxia Zheng, Chun Zeng, Quan Chen, Aimin Zhou Jul 2012

6-Hydroximino-4-Aza-A-Homo-Cholest-3-One And Related Analogue As A Potent Inducer Of Apoptosis In Cancer Cells, Yanmin Huang, Jianguo Cui, Qiaoxia Zheng, Chun Zeng, Quan Chen, Aimin Zhou

Chemistry Faculty Publications

Here we report that 6-hydroximino-4-aza-A-homo-cholest-3-one and 6-hydroxyl-4-aza-A-homo-cholest-3-one, new steroidal lactams were synthesized recently, displayed antiproliferative activity against some cancer cells through inducing cancer cell apoptosis by activation of the intrinsic pathway. The apoptotic function of the compounds was demonstrated by release of cytochrome C, activation of caspase 3 and annexin V labeling. Furthermore, the compound was able to inhibit tumor growth in an athymic mouse model.


Maxwell's Equations, Part Vii, David W. Ball Jun 2012

Maxwell's Equations, Part Vii, David W. Ball

Chemistry Faculty Publications

This is the seventh (and perhaps last) installment of a series of columns on Maxwell’s equations of electrodynamics. In previous columns (available at Spectroscopy’s website, www.spectroscopyonline.com/The+Baseline+Column), we have covered history, the background of the first three equations, and the mathematics underlying them. Here we will present the fourth equation, and after reaching it we’ll see how light is described in terms of these four mathematical expressions.


Insufficient Radiofrequency Ablation Promotes Angiogenesis Of Residual Hepatocellular Carcinoma Via Hif-1Α/Vegfa, Jian Kong, Jinge Kong, Bing Pan, Shan Ke, Shuying Dong, Xiuli Li, Aimin Zhou, Lemin Zheng, Wen Bing Sun May 2012

Insufficient Radiofrequency Ablation Promotes Angiogenesis Of Residual Hepatocellular Carcinoma Via Hif-1Α/Vegfa, Jian Kong, Jinge Kong, Bing Pan, Shan Ke, Shuying Dong, Xiuli Li, Aimin Zhou, Lemin Zheng, Wen Bing Sun

Chemistry Faculty Publications

Background: The mechanism of rapid growth of the residual tumor after radiofrequency (RF) ablation is poorly understood. In this study, we investigated the effect of hyperthermia on HepG2 cells and generated a subline with enhanced viability and dys-regulated angiogenesis in vivo, which was used as a model to further determine the molecular mechanism of the rapid growth of residual HCC after RF ablation. Methodology/Principal Findings: Heat treatment was used to establish sublines of HepG2 cells. A subline (HepG2 k) with a relatively higher viability and significant heat tolerance was selected. The cellular protein levels of VEGFA, HIF-1α and p-Akt, VEGFA …


Introducing Nob-Nobs: Nitrogen-Oxygen-Boron Cycles With Potential High-Energy Properties, Aloysus K. Lawong, David W. Ball May 2012

Introducing Nob-Nobs: Nitrogen-Oxygen-Boron Cycles With Potential High-Energy Properties, Aloysus K. Lawong, David W. Ball

Chemistry Faculty Publications

As a follow-up on a study of a family of boron-oxygen-nitrogen compounds composed of two datively bonded B–O–N backbones, we investigate a similar series of compounds that have similar fragments but are covalently bonded. B3LYP/6-31G(d,p) quantum mechanical calculations have been performed to determine the minimum-energy geometries, vibrational frequencies, and thermochemical properties of the parent compound and a series of nitro-substituted derivatives. Our results indicate that some of the derivatives have at least appropriate thermodynamics for possible high-energy materials, in some cases being favorable over similar dimeric compounds with coordinate covalent B–N bonds


Human Sperm Dna Oxidation, Motility And Viability In The Presence Of L-Carnitine During In Vitro Incubation And Centrifugation, S. Banihani, R. Sharma, Mekki Bayachou, E. Sabanegh, A. Agarwal May 2012

Human Sperm Dna Oxidation, Motility And Viability In The Presence Of L-Carnitine During In Vitro Incubation And Centrifugation, S. Banihani, R. Sharma, Mekki Bayachou, E. Sabanegh, A. Agarwal

Chemistry Faculty Publications

In vitro incubation and centrifugation is known to decrease human sperm quality. In the human body, besides its antioxidant effects, l-carnitine (LC) facilitates the transport of activated fatty acids from the cytosol to the mitochondrial matrix. In this study, we investigated the effect of LC on human sperm motility, viability and DNA oxidation after incubation and centrifugation, following the sperm preparation protocols of assisted reproduction. Normozoospermic semen samples (n = 55) were analysed according to the World Health Organization (WHO) guidelines. LC concentrations that are not toxic to spermatozoa as determined by sperm motility and viability were standardised after 2 …


Bon-Bons: Cyclic Molecules With A Boron-Oxygen-Nitrogen Backbone. Computational Studies Of Their Thermodynamic Properties, Aloysus K. Lawong, David W. Ball Apr 2012

Bon-Bons: Cyclic Molecules With A Boron-Oxygen-Nitrogen Backbone. Computational Studies Of Their Thermodynamic Properties, Aloysus K. Lawong, David W. Ball

Chemistry Faculty Publications

Although they were first reported in 1963, molecules with a boron-oxygen-nitrogen dimeric backbone do not seem to have been investigated seriously in terms of thermodynamic properties. Here we report on the calculated structures and properties, including thermodynamics, of several so-called “BON-BON” molecules. With the popularity of nitrogen-containing substituents on new high-energy materials, nitro-substituted BON-BONs were a focus of our investigation. A total of 42 BON-BON molecules were evaluated, and thermochemical analysis shows a decrease in the specific enthalpy of combustion or decomposition with increasing NO2 content, consistent with other systems.


Probe Functionalization With A Rhop-3 Antibody: Toward A Rhop-3 Antigen Immunosensor For Detection Of Malaria, Salaam Saleh, Susan Moreno Molek, Perera N. Indika, Alan Riga, Tobili Sam Yellowe, Mekki Bayachou Mar 2012

Probe Functionalization With A Rhop-3 Antibody: Toward A Rhop-3 Antigen Immunosensor For Detection Of Malaria, Salaam Saleh, Susan Moreno Molek, Perera N. Indika, Alan Riga, Tobili Sam Yellowe, Mekki Bayachou

Chemistry Faculty Publications

The antibody specific for the malaria protein, Rhop-3, and FL-Rhop-3, were immobilized on the surface of a gold electrode modified with cysteamine. Colloidal gold was used to enhance the detection signal for Rhop-3 antigens. The Rhop-3 antibody was also immobilized on gold electrodes preactivated with dithiobis(succinimidyl proprionate) (DSP). Immobilization was performed at room temperature and at 37 °C. Cyclic voltammetry (CV) was used to monitor the interaction between the immobilized antibody and its cognate antigen in solution, using ferricyanide, K3Fe(CN)6, as reporting electroactive probe. Tests indicate recognition of Rhop-3 protein by the immobilized antibody. Antigen recognition was enhanced by incubation …


From Cox-2 Inhibitor Nimesulide To Potent Anti-Cancer Agent: Synthesis, In Vitro, In Vivo And Pharmacokinetic Evaluation, Bo Zhong, Xiaohan Cai, Snigdha Chennamaneni, Xin Yi, Lili Liu, John J. Pink, Afshin Dowlati, Yan Xu, Aimin Zhou, Bin Su Jan 2012

From Cox-2 Inhibitor Nimesulide To Potent Anti-Cancer Agent: Synthesis, In Vitro, In Vivo And Pharmacokinetic Evaluation, Bo Zhong, Xiaohan Cai, Snigdha Chennamaneni, Xin Yi, Lili Liu, John J. Pink, Afshin Dowlati, Yan Xu, Aimin Zhou, Bin Su

Chemistry Faculty Publications

Cyclooxygenase-2 (COX-2) inhibitor nimesulide inhibits the proliferation of various types of cancer cells mainly via COX-2 independent mechanisms, which makes it a good lead compound for anti-cancer drug development. In the presented study, a series of new nimesulide analogs were synthesized based on the structure–function analysis generated previously. Some of them displayed very potent anti-cancer activity with IC50s around 100 nM–200 nM to inhibit SKBR-3 breast cancer cell growth. CSUOH0901 (NSC751382) from the compound library also inhibits the growth of the 60 cancer cell lines used at National Cancer Institute Developmental therapeutics Program (NCIDTP) with IC50s around 100 nM–500 nM. …


Characterization Of Pharmaceutical Materials By Thermal And Analytical Methods, Manik Pavan Kumar Maheswaram Jan 2012

Characterization Of Pharmaceutical Materials By Thermal And Analytical Methods, Manik Pavan Kumar Maheswaram

ETD Archive

No abstract provided.


Design And Synthesis Of Antithrombotic Liposomal Protein Conjugate, Hailong Zhang Jan 2012

Design And Synthesis Of Antithrombotic Liposomal Protein Conjugate, Hailong Zhang

ETD Archive

Recent advances in the molecular bases of haemostasis have highlighted that endothelial thrombomodulin (TM) plays a critical role in local haemostasis by binding thrombin and subsequently converting protein C to its active form (APC). In addition, the binding of thrombin to TM drastically alters the thrombin's procoagulant activities to anticoagulant activities. The lipid bilayer in which it resides serves as an essential 'cofactor', locally concentrating and coordinating the appropriate alignment of reacting cofactors and substrates for protein C activation. On the other hand, liposomes have been extensively studied as cell membrane model as well as carrier for delivering certain vaccines, …


Novel Solid State Properties Of Drugs, Polymers And Various Chemicals By Thermal And Analytical Techniques, Dhruthiman R. Mantheni Jan 2012

Novel Solid State Properties Of Drugs, Polymers And Various Chemicals By Thermal And Analytical Techniques, Dhruthiman R. Mantheni

ETD Archive

I have observed unique variations in AC electrical conductivity of solids by dielectric analysis (DEA or DETA) when studied with respect to temperature and frequency. A wide range of solids were examined for this study e.g. organics, polymers, carbohydrates, API's (active pharmacy ingredients) and amino acids. Experimental results clearly show novel dielectric behavior of a linear increase in a log ionic conductivity vs. temperature in the pre-melt (20 to 30oC below the melt temperature) and melt transition regions. We have differentiated the solids which show the conductivity variations in pre-melt from those which do not e.g. pre-melt conductivity variations observed …


Development Of A ‘Clickable’ Non-Natural Nucleotide To Visualize The Replication Of Non-Instructional Dna Lesions, Edward A. Motea, Irene Lee, Anthony J. Berdis Jan 2012

Development Of A ‘Clickable’ Non-Natural Nucleotide To Visualize The Replication Of Non-Instructional Dna Lesions, Edward A. Motea, Irene Lee, Anthony J. Berdis

Chemistry Faculty Publications

The misreplication of damaged DNA is an important biological process that produces numerous adverse effects on human health. This report describes the synthesis and characterization of a non-natural nucleotide, designated 3-ethynyl-5-nitroindolyl-2′-deoxyriboside triphosphate (3-Eth-5-NITP), as a novel chemical reagent that can probe and quantify the misreplication of damaged DNA. We demonstrate that this non-natural nucleotide is efficiently inserted opposite an abasic site, a commonly formed and potentially mutagenic non-instructional DNA lesion. The strategic placement of the ethynyl moiety allows the incorporated nucleoside triphosphate to be selectively tagged with an azide-containing fluorophore using ‘click’ chemistry. This reaction provides a facile way to …