Open Access. Powered by Scholars. Published by Universities.®

Digital Commons Network™

Open Access. Powered by Scholars. Published by Universities.®

University of Rhode Island

Discipline
Keyword
Publication Year
Publication
Publication Type
File Type

Articles 3961 - 3990 of 7472

Full-Text Articles in Entire DC Network

3-Substitued Indoles: One-Pot Synthesis And Evaluation Of Anticancer And Src Kinase Inhibitory Activities, K. Kameshwara Rao, Bhupender S. Chhikara, Amir Nasrolahi Shirazi, Rakesh Tiwari, Keykavous Parang, Anil Kumar Jan 2011

3-Substitued Indoles: One-Pot Synthesis And Evaluation Of Anticancer And Src Kinase Inhibitory Activities, K. Kameshwara Rao, Bhupender S. Chhikara, Amir Nasrolahi Shirazi, Rakesh Tiwari, Keykavous Parang, Anil Kumar

Biomedical and Pharmaceutical Sciences Faculty Publications

An efficient and economical method was developed for the synthesis of 3-substituted indoles by one-pot three-component coupling reaction of a substituted or unsubstituted benzaldehyde, N-methylaniline, and indole or N-methylindole using Yb(OTf)3–SiO2 as a catalyst. All the synthesized compounds were evaluated for inhibition of cell proliferation of human colon carcinoma (HT-29), human ovarian adenocarcinoma (SK-OV-3), and c-Src kinase activity. The 4-methylphenyl (4o and 4p) and 4-methoxyphenyl (4q) indole derivatives inhibited the cell proliferation of SK-OV-3 and HT-29 cells by 70–77% at a concentration of 50 μM. The unsubstituted phenyl (4d) …


Half-Sandwich Ruthenium–Arene Complexes With Thiosemicarbazones: Synthesis And Biological Evaluation Of [(Η6-P-Cymene)Ru(Piperonal Thiosemicarbazones)Cl]Cl Complexes, Floyd Beckford, Deidra Dourth, Michael Shaloski Jr., Jacob Didion, Jeffrey Thessing, Jason Woods, Vernon Crowell, Nikolay Gerasimchuk, Antonio Gonzalez-Sarrías, Navindra P. Seeram Jan 2011

Half-Sandwich Ruthenium–Arene Complexes With Thiosemicarbazones: Synthesis And Biological Evaluation Of [(Η6-P-Cymene)Ru(Piperonal Thiosemicarbazones)Cl]Cl Complexes, Floyd Beckford, Deidra Dourth, Michael Shaloski Jr., Jacob Didion, Jeffrey Thessing, Jason Woods, Vernon Crowell, Nikolay Gerasimchuk, Antonio Gonzalez-Sarrías, Navindra P. Seeram

Biomedical and Pharmaceutical Sciences Faculty Publications

The synthesis and characterization of a number of organometallic ruthenium(II) complexes containing a series of bidentate thiosemicarbazone ligands derived from piperonal is reported. The structure of compounds have been confirmed by spectroscopic analysis (IR and NMR) as well as X-ray crystallographic analysis of [(η6-p-cymene)Ru(pPhTSC)Cl]Cl (4) (pPhTSC is piperonal-N(4)-phenylthiosemicarbazone). The interaction of the complexes ([(η6-p-cymene)Ru(pEtTSC)Cl]Cl) (3) (pEtTSC is piperonal-N(4)-ethylthiosemicarbazone) and 4 with calf thymus DNA, human serum albumin (HSA) and pBR322 plasmid DNA were studied by spectroscopic, gel electrophoresis and hydrodynamic methods. The apparent binding constant for the interaction …


Division Of Research And Economic Development Annual Report For Fy2011, Uri Division Of Research And Economic Development Jan 2011

Division Of Research And Economic Development Annual Report For Fy2011, Uri Division Of Research And Economic Development

Reports (Research and Economic Development)

Annual report for the Division of Research and Economic Development of the University of Rhode Island for the year 2010-2011.

Includes statistics of project proposals, expenditures, URI Foundation Awards, previous annual report summaries and awards received by individual academic and administrative departments.


Division Of Research And Economic Development Monthly Report For February 2011, Uri Division Of Research And Economic Development Jan 2011

Division Of Research And Economic Development Monthly Report For February 2011, Uri Division Of Research And Economic Development

Reports (Research and Economic Development)

The monthly reports include statistics for project proposals and awards received by individual academic and administrative departments at the University of Rhode Island.


Division Of Research And Economic Development Monthly Report For March 2011, Uri Division Of Research And Economic Development Jan 2011

Division Of Research And Economic Development Monthly Report For March 2011, Uri Division Of Research And Economic Development

Reports (Research and Economic Development)

The monthly reports include statistics for project proposals and awards received by individual academic and administrative departments at the University of Rhode Island.


Division Of Research And Economic Development Monthly Report For January 2011, Uri Division Of Research And Economic Development Jan 2011

Division Of Research And Economic Development Monthly Report For January 2011, Uri Division Of Research And Economic Development

Reports (Research and Economic Development)

The monthly reports include statistics for project proposals and awards received by individual academic and administrative departments at the University of Rhode Island.


Division Of Research And Economic Development Monthly Report For April-May 2011, Uri Division Of Research And Economic Development Jan 2011

Division Of Research And Economic Development Monthly Report For April-May 2011, Uri Division Of Research And Economic Development

Reports (Research and Economic Development)

The monthly reports include statistics for project proposals and awards received by individual academic and administrative departments at the University of Rhode Island.


Division Of Research And Economic Development Monthly Report For December 2011, Uri Division Of Research And Economic Development Jan 2011

Division Of Research And Economic Development Monthly Report For December 2011, Uri Division Of Research And Economic Development

Reports (Research and Economic Development)

The monthly reports include statistics for project proposals and awards received by individual academic and administrative departments at the University of Rhode Island.


Division Of Research And Economic Development Monthly Report For October-November 2011, Uri Division Of Research And Economic Development Jan 2011

Division Of Research And Economic Development Monthly Report For October-November 2011, Uri Division Of Research And Economic Development

Reports (Research and Economic Development)

The monthly reports include statistics for project proposals and awards received by individual academic and administrative departments at the University of Rhode Island.


Division Of Research And Economic Development Monthly Report For July-September 2011, Uri Division Of Research And Economic Development Jan 2011

Division Of Research And Economic Development Monthly Report For July-September 2011, Uri Division Of Research And Economic Development

Reports (Research and Economic Development)

The monthly reports include statistics for project proposals and awards received by individual academic and administrative departments at the University of Rhode Island.


Coupling Sensitive In Vitro And In Silico Techniques To Assess Cross-Reactive Cd4+ T Cells Against The Swine-Origin H1n1 Influenza Virus, Brian C. Schanen, Anne S. De Groot, Leonard Moise, Matt Ardito, Elizabeth Mcclaine, William Martin, Vaughan Wittman, William L. Warren, Donald R. Drake Iii Jan 2011

Coupling Sensitive In Vitro And In Silico Techniques To Assess Cross-Reactive Cd4+ T Cells Against The Swine-Origin H1n1 Influenza Virus, Brian C. Schanen, Anne S. De Groot, Leonard Moise, Matt Ardito, Elizabeth Mcclaine, William Martin, Vaughan Wittman, William L. Warren, Donald R. Drake Iii

Institute for Immunology and Informatics Faculty Publications

The outbreak of the novel swine-origin H1N1 influenza in the spring of 2009 took epidemiologists, immunologists, and vaccinologists by surprise and galvanized a massive worldwide effort to produce millions of vaccine doses to protect against this single virus strain. Of particular concern was the apparent lack of pre-existing antibody capable of eliciting cross-protective immunity against this novel virus, which fueled fears this strain would trigger a particularly far-reaching and lethal pandemic. Given that disease caused by the swine-origin virus was far less severe than expected, we hypothesized cellular immunity to cross-conserved T cell epitopes might have played a significant role …


Helicovax: Epitope-Based Therapeutic Helicobacter Pylori Vaccination In A Mouse Model, Steven F. Moss, Leonard Moise, Dong Soo Lee, Woojin Kim, Songhua Zhang, Jinhee Lee, Arlin B. Rogers, William Martin, Anne S. De Groot Jan 2011

Helicovax: Epitope-Based Therapeutic Helicobacter Pylori Vaccination In A Mouse Model, Steven F. Moss, Leonard Moise, Dong Soo Lee, Woojin Kim, Songhua Zhang, Jinhee Lee, Arlin B. Rogers, William Martin, Anne S. De Groot

Institute for Immunology and Informatics Faculty Publications

Helicobacter pylori is the leading cause of gastritis, peptic ulcer disease and gastric adenocarcinoma and lymphoma in humans. Due to the decreasing efficacy of anti-H. pylori antibiotic therapy in clinical practice, there is renewed interest in the development of anti-H. pylori vaccines. In this study an in silico-based approach was utilized to develop a multi-epitope DNA-prime/peptide-boost immunization strategy using informatics tools. The efficacy of this construct was then assessed as a therapeutic vaccine in a mouse model of gastric cancer induced by chronic H. pylori infection. The multi-epitope vaccine administered intranasally induced a broad immune response as determined …


Harnessing The Power Of Genomics And Immunoinformatics To Produce Improved Vaccines, Leonard Moise, Leslie Cousens, Joanna Fueyo, Anne S. De Groot Jan 2011

Harnessing The Power Of Genomics And Immunoinformatics To Produce Improved Vaccines, Leonard Moise, Leslie Cousens, Joanna Fueyo, Anne S. De Groot

Institute for Immunology and Informatics Faculty Publications

The role of cellular immunity as a mediator of protection against disease is gaining recognition, particularly with regard to the many pathogens for which we presently lack effective vaccines. As a result, there is an ever-increasing need to understand the T-cell populations induced by vaccination and, therefore, T-cell epitopes responsible for triggering their activation. Although the characterization and harnessing of cellular immunity for vaccine development is an active area of research interest, the field still needs to rigorously define T-cell epitope specificities, above all, on a genomic level. New immunoinformatic epitope mapping tools now make it possible to identify pathogen …


Expression Of The Distalless-B Gene In Ciona Is Regulated By A Pan-Ectodermal Enhancer Module, Steven Q. Irvine, David A. Vierra, Brad J. Millette, Matthew D. Blanchette, Rachel E. Holbert Jan 2011

Expression Of The Distalless-B Gene In Ciona Is Regulated By A Pan-Ectodermal Enhancer Module, Steven Q. Irvine, David A. Vierra, Brad J. Millette, Matthew D. Blanchette, Rachel E. Holbert

Biological Sciences Faculty Publications

The Ci-Dll-B gene is an early regulator of ectodermal development in the ascidian Ciona intestinalis (Imai et al., 2006). Ci-Dll-B is located in a convergently transcribed bigene cluster with a tandem duplicate, Ci-Dll-A. This clustered genomic arrangement is the same as those of the homologous vertebrate Dlx genes, which are also arranged in convergently transcribed bigene clusters. Sequence analysis of the C. intestinalis Dll-A-B cluster reveals a 378 bp region upstream of Ci-Dll-B, termed B1, which is highly conserved with the corresponding region from the congener Ciona savignyi. The B1 element is necessary and sufficient to …


Gender And Women's Studies Newsletter For Spring 2011, Uri Gender And Women's Studies Department Jan 2011

Gender And Women's Studies Newsletter For Spring 2011, Uri Gender And Women's Studies Department

Gender and Women's Studies Publications

The Spring 2011 issue of Gender and Women’s Studies Newsletter, a periodical with articles written by faculty members and some related to events within the Gender and Women’s Studies program.


Modeling Habitat Associations For The Common Loon (Gavia Immer) At Multiple Scales In Northeastern North America, Anne Kuhn, Jane Copeland, John Cooley, Harry Vogel, Kate Taylor, Diane Nacci, Peter V. August Jan 2011

Modeling Habitat Associations For The Common Loon (Gavia Immer) At Multiple Scales In Northeastern North America, Anne Kuhn, Jane Copeland, John Cooley, Harry Vogel, Kate Taylor, Diane Nacci, Peter V. August

Natural Resources Science Faculty Publications

Common Loon (Gavia immer) is considered an emblematic and ecologically important example of aquatic-dependent wildlife in North America. The northern breeding range of Common Loon has contracted over the last century as a result of habitat degradation from human disturbance and lakeshore development. We focused on the state of New Hampshire, USA, where a long-term monitoring program conducted by the Loon Preservation Committee has been collecting biological data on Common Loon since 1976. The Common Loon population in New Hampshire is distributed throughout the state across a wide range of lake-specific habitats, water quality conditions, and levels of …


Nonnative Phragmites Australis Invasion Into Utah Wetlands, Andrew Kulmatiski, Karen H. Beard, Laura A. Meyerson, Jacob R. Gibson, Karen E. Mock Jan 2011

Nonnative Phragmites Australis Invasion Into Utah Wetlands, Andrew Kulmatiski, Karen H. Beard, Laura A. Meyerson, Jacob R. Gibson, Karen E. Mock

Natural Resources Science Faculty Publications

Phragmites australis (Cav.) Trin. ex Steud. (common reed), already one of the world's most widespread plant species, has realized rapid range expansion in coastal wetlands of North America in the past century, but little is known about P. australis range expansion in inland wetland systems. We used genetic analyses, aerial photographs, field surveys, and a greenhouse experiment to study the extent and mechanism of nonnative P. australis invasion of Utah wetlands. We collected and genetically analyzed 39 herbarium samples across the state and 225 present-day samples from northern Utah's major wetland complexes. All samples collected before 1993 and all samples …


A Mass Balance Approach To Identify And Compare Differential Routing Of 13C-Labeled Carbohydrates, Lipids, And Proteins In Vivo, Marshall D. Mccue, Adam Smith, Richard Mckinney, Boris Rewald, Berry Pinshow, Scott R. Mcwilliams Jan 2011

A Mass Balance Approach To Identify And Compare Differential Routing Of 13C-Labeled Carbohydrates, Lipids, And Proteins In Vivo, Marshall D. Mccue, Adam Smith, Richard Mckinney, Boris Rewald, Berry Pinshow, Scott R. Mcwilliams

Natural Resources Science Faculty Publications

All animals route assimilated nutrients to their tissues where they are used to support growth or are oxidized for energy. These nutrients are probably not allocated homogeneously among the various tissue and are more likely to be preferentially routed toward some tissues and away from others. Here we introduce an approach that allows researchers to identify and compare nutrient routing among different organs and tissues. We tested this approach by examining nutrient routing in birds. House sparrows Passer domesticus were fed a meal supplemented with one of seven 13C-labeled metabolic tracers representing three major classes of macronutrients, namely, carbohydrates, …


Maintaining Exercise And Healthful Eating In Older Adults: The Senior Project Ii: Study Design And Methodology, Phillip G. Clark, Bryan J. Blissmer, Geoffrey W. Greene, Faith D. Lees, Deborah A. Riebe, Karen E. Stamm Jan 2011

Maintaining Exercise And Healthful Eating In Older Adults: The Senior Project Ii: Study Design And Methodology, Phillip G. Clark, Bryan J. Blissmer, Geoffrey W. Greene, Faith D. Lees, Deborah A. Riebe, Karen E. Stamm

Nutrition Faculty Publications

The Study of Exercise and Nutrition in Older Rhode Islanders (SENIOR) Project II is an intervention study to promote the maintenance of both exercise and healthful eating in older adults. It is the second phase of an earlier study, SENIOR Project I, that originally recruited 1277 community-dwelling older adults to participate in behavior-specific interventions designed to increase exercise and/or fruit and vegetable consumption. The general theoretical framework for this research is the Transtheoretical Model (TTM) of Health Behavior Change.

The current intervention occurs over a 48-month period, using a manual, newsletters, and phone coaching calls. Annual assessments collect standardized data …


Surfo Technical Report No. 11-01, Surfo Jan 2011

Surfo Technical Report No. 11-01, Surfo

SURFO Technical Reports

The 2011 technical reports written by undergraduate students participating in the SURFO (Summer Undergraduate Research Fellowships in Oceanography) Program while at the University of Rhode Island.


Research & Innovation For 2010-2011, University Of Rhode Island Jan 2011

Research & Innovation For 2010-2011, University Of Rhode Island

Publications (Research and Economic Development)

The 2010-2011 issue of Research & Innovation, a periodical focused on research at the University of Rhode Island.


Monitoring Nonenzymatic Glycation Of Human Immunoglobulin G By Methylglyoxal And Glyoxal: A Spectroscopic Study, Praveen K. Pampati, Sreekanth Suravajjala, Joel A. Dain Jan 2011

Monitoring Nonenzymatic Glycation Of Human Immunoglobulin G By Methylglyoxal And Glyoxal: A Spectroscopic Study, Praveen K. Pampati, Sreekanth Suravajjala, Joel A. Dain

Chemistry Faculty Publications

The accumulation of dicarbonyl compounds, methylglyoxal (MG) and glyoxal (G), has been observed in diabetic conditions. They are formed from nonoxidative mechanisms in anaerobic glycolysis and lipid peroxidation, and they act as advanced glycation endproduct (AGE) precursors. The objective of this study was to monitor and characterize the AGE formation of human immunoglobulin G (hIgG) by MG and G using ultraviolet (UV) and fluorescence spectroscopy, circular dichroism (CD), and matrix-assisted laser desorption/ionization–mass spectrometry (MALDI–MS). hIgG was incubated over time with MG and G at different concentrations. Formation of AGE was monitored by UV and fluorescence spectroscopy. The effect of AGE …


Baseline Stage, Severity, And Effort Effects Differentiate Stable Smokers From Maintainers And Relapsers, Colleen A. Redding, James O. Prochaska, Andrea L. Paiva, Joseph S. Rossi, Wayne F. Velicer, Bryan J. Blissmer, Geoffrey W. Greene, Mark L. Robbins, Xiaowu Sun Jan 2011

Baseline Stage, Severity, And Effort Effects Differentiate Stable Smokers From Maintainers And Relapsers, Colleen A. Redding, James O. Prochaska, Andrea L. Paiva, Joseph S. Rossi, Wayne F. Velicer, Bryan J. Blissmer, Geoffrey W. Greene, Mark L. Robbins, Xiaowu Sun

Cancer Prevention Research Center Faculty Publications

This cross-sectional study (N = 4,144) compared three longitudinal dynatypes (Maintainers, Relapsers, and Stable Smokers) of smokers on baseline demographics, stage, addiction severity, and transtheoretical model effort effect variables. There were significant small-to-medium-sized differences between the Stable Smokers and the other two groups on stage, severity, and effort effect variables in both treatment and control groups. There were few significant, very small differences on baseline effort variables between Maintainers and Relapsers in the control, but not the treatment group. The ability to identify Stable Smokers at baseline could permit enhanced tailored treatments that could improve population cessation rates.


Phenol Nitration Induced By An {Fe(No)2}10 Dinitrosyl Iron Complex, Nhut Giuc Tran, Harris Kalyvas, Kelsey M. Skodje, Takahiro Hayashi, Pierre Moënne-Loccoz, Jason Shearer, Louis J. Kirschenbaum, Eunsuk Kim Jan 2011

Phenol Nitration Induced By An {Fe(No)2}10 Dinitrosyl Iron Complex, Nhut Giuc Tran, Harris Kalyvas, Kelsey M. Skodje, Takahiro Hayashi, Pierre Moënne-Loccoz, Jason Shearer, Louis J. Kirschenbaum, Eunsuk Kim

Chemistry Faculty Publications

Cellular dinitrosyl iron complexes (DNICs) have long been considered NO carriers. Although other physiological roles of DNICs have been postulated, their chemical functionality outside of NO transfer has not been demonstrated thus far. Here we report the unprecedented dioxygen reactivity of a N-bound {Fe(NO)2}10 DNIC, [Fe(TMEDA)(NO)2] (1). In the presence of O2, 1 becomes a nitrating agent that converts 2,4,-di-tert-butylphenol to 2,4-di-tert-butyl-6-nitrophenol via formation of a putative iron-peroxynitrite [Fe(TMEDA)(NO)(ONOO)] (2) that is stable below −80 °C. Iron K-edge X-ray absorption spectroscopy on 2 supports a …


Analysis Of Sustainable Pest Control Using A Pesticide And A Screened Refuge, John Ringland, Prasanth George Jan 2011

Analysis Of Sustainable Pest Control Using A Pesticide And A Screened Refuge, John Ringland, Prasanth George

Mathematics Faculty Publications

We describe and analyze a ‘screened refuge’ technique for indefinitely sustaining control of insect pests using transgenic pesticidal crops or an applied pesticide, even when resistance is not recessive. The screen is a physical barrier that restricts pest movement. In a deterministic discrete‐time model of the use of this technique, we obtain asymptotic analytical formulas for the two important equilibria of the system in terms of the refuge size and the pest fitnesses, mutation rates, and mobility out of and into the refuge. One of the equilibria is stable and is the point at which the pest population is controlled. …


Bioassays Of Analogs Of Pleurocidin-Amide Indicate That Change At N-Terminus Is Key To Improved Efficacy, Roxanne Lacroix, Krishna Tamminedi, David E. Ryder, Jay F. Sperry, Lenore M. Martin Jan 2011

Bioassays Of Analogs Of Pleurocidin-Amide Indicate That Change At N-Terminus Is Key To Improved Efficacy, Roxanne Lacroix, Krishna Tamminedi, David E. Ryder, Jay F. Sperry, Lenore M. Martin

Cell and Molecular Biology Faculty Publications

No abstract provided.


Synthesis And Characterization Of Mixed-Ligand Diimine-Piperonal Thiosemicarbazone Complexes Of Ruthenium(Ii): Biophysical Investigations And Biological Evaluation As Anticancer And Antibacterial Agents, Floyd A. Beckford, Jeffrey Thessing, Michael Shaloski Jr., P. Canisius Mbarushimana, Alyssa Brock, Jacob Didion, Jason Woods, Antonio Gonzalez-Sarrías, Navindra P. Seeram Jan 2011

Synthesis And Characterization Of Mixed-Ligand Diimine-Piperonal Thiosemicarbazone Complexes Of Ruthenium(Ii): Biophysical Investigations And Biological Evaluation As Anticancer And Antibacterial Agents, Floyd A. Beckford, Jeffrey Thessing, Michael Shaloski Jr., P. Canisius Mbarushimana, Alyssa Brock, Jacob Didion, Jason Woods, Antonio Gonzalez-Sarrías, Navindra P. Seeram

Biomedical and Pharmaceutical Sciences Faculty Publications

We have used a novel microwave-assisted method developed in our laboratories to synthesize a series of ruthenium-thiosemicarbazone complexes. The new thiosemicarbazone ligands are derived from benzo[d][1,3]dioxole-5-carbaldehyde (piperonal) and the complexes are formulated as [(diimine)2Ru(TSC)](PF6)2 (where the TSC is the bidentate thiosemicarbazone ligand). The diimine in the complexes is either 2,2′-bipyridine or 1,10-phenanthroline. The complexes have been characterized by spectroscopic means (NMR, IR and UV–Vis) as well as by elemental analysis. We have studied the biophysical characteristics of the complexes by investigating their anti-oxidant ability as well as their ability to disrupt the function …


Vennvax, A Dna-Prime, Peptide-Boost Multi-T-Cell Epitope Poxvirus Vaccine, Induces Protective Immunity Against Vaccinia Infection By T Cell Response Alone, Leonard Moise, R. Mark Buller, Jill Schriewer, Jinhee Lee, Sharon E. Frey, David B. Weiner, William Martin, Anne S. De Groot Jan 2011

Vennvax, A Dna-Prime, Peptide-Boost Multi-T-Cell Epitope Poxvirus Vaccine, Induces Protective Immunity Against Vaccinia Infection By T Cell Response Alone, Leonard Moise, R. Mark Buller, Jill Schriewer, Jinhee Lee, Sharon E. Frey, David B. Weiner, William Martin, Anne S. De Groot

Institute for Immunology and Informatics Faculty Publications

The potential for smallpox to be disseminated in a bioterror attack has prompted development of new, safer smallpox vaccination strategies. We designed and evaluated immunogenicity and efficacy of a T-cell epitope vaccine based on conserved and antigenic vaccinia/variola sequences, identified using bioinformatics and immunological methods. Vaccination in HLA transgenic mice using a DNA-prime/peptide-boost strategy elicited significant T cell responses to multiple epitopes. No antibody response pre-challenge was observed, neither against whole vaccinia antigens nor vaccine epitope peptides. Remarkably, 100% of vaccinated mice survived lethal vaccinia challenge, demonstrating that protective immunity to vaccinia does not require B cell priming.


Click Chemistry Inspired One-Pot Synthesis Of 1,4-Disubstituted 1,2,3-Triazoles And Their Src Kinase Inhibitory Activity, Dalip Kumar, V. Buchi Reddy, Anil Kumar, Deendayal Mandal, Rakesh Tiwari, Keykavous Parang Jan 2011

Click Chemistry Inspired One-Pot Synthesis Of 1,4-Disubstituted 1,2,3-Triazoles And Their Src Kinase Inhibitory Activity, Dalip Kumar, V. Buchi Reddy, Anil Kumar, Deendayal Mandal, Rakesh Tiwari, Keykavous Parang

Biomedical and Pharmaceutical Sciences Faculty Publications

Two classes of 1,4-disubstituted 1,2,3-triazoles were synthesized using one-pot reaction of α-tosyloxy ketones/α-halo ketones, sodium azide, and terminal alkynes in the presence of aq PEG (1:1, v/v) using the click chemistry approach and evaluated for Src kinase inhibitory activity. Structure–activity relationship analysis demonstrated that insertion of C6H5– and 4-CH3C6H4– at position 4 for both classes and less bulkier aromatic group at position 1 in class 1 contribute critically to the modest Src inhibition activity (IC50 = 32–43 μM) of 1,4-disubstituted 1,2,3-triazoles.

[Refer to PDF for graphical abstract]


Metal-Free Intermolecular Oxidative C–N Bond Formation Via Tandem C–H And N–H Bond Functionalization, Abhishek A. Kantak, Shathaverdhan Potavathri, Rose A. Barham, Kaitlyn M. Romano, Brenton Deboef Jan 2011

Metal-Free Intermolecular Oxidative C–N Bond Formation Via Tandem C–H And N–H Bond Functionalization, Abhishek A. Kantak, Shathaverdhan Potavathri, Rose A. Barham, Kaitlyn M. Romano, Brenton Deboef

Chemistry Faculty Publications

The development of a novel intermolecular oxidative amination reaction, a synthetic transformation that involves the simultaneous functionalization of both a N–H and C–H bond, is described. The process, which is mediated by an I(III) oxidant and contains no metal catalysts, provides a rapid and green method for synthesizing protected anilines from simple arenes and phthalimide. Mechanistic investigations indicate that the reaction proceeds via nucleophilic attack of the phthalimide on an aromatic radical cation, as opposed to the electrophilic aromatic amination that has been reported for other I(III) amination reactions. The application of this new reaction to the synthesis of a …