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Route Exploration And Synthesis Of The Reported Pyridone-Based Pdi Inhibitor Stk076545, Eric Greve, Sergey V. Lindeman, Christina Scartelli, Lin Lin, Robert Flaumenhaft, Chris Dockendorff
Route Exploration And Synthesis Of The Reported Pyridone-Based Pdi Inhibitor Stk076545, Eric Greve, Sergey V. Lindeman, Christina Scartelli, Lin Lin, Robert Flaumenhaft, Chris Dockendorff
Chemistry Faculty Research and Publications
The enzyme protein disulfide isomerase (PDI) is essential for the correct folding of proteins and the activation of certain cell surface receptors, and is a promising target for the treatment of cancer and thrombotic conditions. A previous high-throughput screen identified the commercial compound STK076545 as a promising PDI inhibitor. To confirm its activity and support further biological studies, a resynthesis was pursued of the reported β-keto-amide with an N-alkylated pyridone at the α-position. Numerous conventional approaches were complicated by undesired fragmentations or rearrangements. However, a successful 5-step synthetic route was achieved using an aldol reaction with an α-pyridone allyl …
Synthesis Of Simplified Azasordarin Analogs As Potential Antifungal Agents, Yibiao Wu, Chris Dockendorff
Synthesis Of Simplified Azasordarin Analogs As Potential Antifungal Agents, Yibiao Wu, Chris Dockendorff
Chemistry Faculty Research and Publications
A new series of simplified azasordarin analogs was synthesized using as key steps a Diels–Alder reaction to generate a highly substituted bicyclo[2.2.1]heptane core, followed by a subsequent nitrile alkylation. Several additional strategies were investigated for the generation of the key tertiary nitrile or aldehyde thought to be required for inhibition at the fungal protein eukaryotic elongation factor 2. This new series also features a morpholino glycone previously reported in semisynthetic sordarin derivatives with broad spectrum antifungal activity. Despite a lack of activity against Candida albicans for these early de novo analogs, the synthetic route reported here permits more comprehensive modifications …
Characterization Of Protease-Activated Receptor (Par) Ligands: Parmodulins Are Reversible Allosteric Inhibitors Of Par1-Driven Calcium Mobilization In Endothelial Cells, Disha M. Gandhi, Mark W. Majewski, Ricardo Rosas Jr., Kaitlin Kentala, Trevor J. Foster, Eric Greve, Chris Dockendorff
Characterization Of Protease-Activated Receptor (Par) Ligands: Parmodulins Are Reversible Allosteric Inhibitors Of Par1-Driven Calcium Mobilization In Endothelial Cells, Disha M. Gandhi, Mark W. Majewski, Ricardo Rosas Jr., Kaitlin Kentala, Trevor J. Foster, Eric Greve, Chris Dockendorff
Chemistry Faculty Research and Publications
Several classes of ligands for Protease-Activated Receptors (PARs) have shown impressive anti-inflammatory and cytoprotective activities, including PAR2 antagonists and the PAR1-targeting parmodulins. In order to support medicinal chemistry studies with hundreds of compounds and to perform detailed mode-of-action studies, it became important to develop a reliable PAR assay that is operational with endothelial cells, which mediate the cytoprotective effects of interest. We report a detailed protocol for an intracellular calcium mobilization assay with adherent endothelial cells in multiwell plates that was used to study a number of known and new PAR1 and PAR2 ligands, including an alkynylated version of the …
Controlled Release Kinetics In Hydroxy Double Salts: Effect Of Host Anion Structure, Stephen Majoni, Jeanne M. Hossenlopp
Controlled Release Kinetics In Hydroxy Double Salts: Effect Of Host Anion Structure, Stephen Majoni, Jeanne M. Hossenlopp
Chemistry Faculty Research and Publications
Nanodimensional layered metal hydroxides such as layered double hydroxides (LDHs) and hydroxy double salts (HDSs) can undergo anion exchange reactions releasing intercalated anions. Because of this, these metal hydroxides have found applications in controlled release delivery of bioactive species such as drugs and pesticides. In this work, isomers of hydroxycinnamate were used as model compounds to systematically explore the effects of anion structure on the rate and extent of anion release in HDSs. Following intercalation and subsequent release of the isomers, it has been demonstrated that the nature and position of substituent groups on intercalated anions have profound effects on …
Reactive Pathways In The Chlorobenzene–Ammonia Dimer Cation Radical: New Insights From Experiment And Theory, Scott A. Reid
Reactive Pathways In The Chlorobenzene–Ammonia Dimer Cation Radical: New Insights From Experiment And Theory, Scott A. Reid
Chemistry Faculty Research and Publications
Building upon our recent studies of noncovalent interactions in chlorobenzene and bromobenzene clusters, in this work we focus on interactions of chlorobenzene (PhCl) with a prototypical N atom donor, ammonia (NH3). Thus, we have obtained electronic spectra of PhCl···(NH3)n (n = 1–3) complexes in the region of the PhCl monomer S0 −S1 (ππ*) transition using resonant 2-photon ionization (R2PI) methods combined with time-of-flight mass analysis. Consistent with previous studies, we find that upon ionization the PhCl···NH3 dimer cation radical reacts primarily via Cl atom loss. A second channel, HCl loss, is …
Β-Diketonate, Β-Ketoiminate, And Β-Diiminate Complexes Of Difluoroboron, Felipe P. Macedo, Chengeto Gwengo, Sergey V. Lindeman, Mark D. Smith, James R. Gardinier
Β-Diketonate, Β-Ketoiminate, And Β-Diiminate Complexes Of Difluoroboron, Felipe P. Macedo, Chengeto Gwengo, Sergey V. Lindeman, Mark D. Smith, James R. Gardinier
Chemistry Faculty Research and Publications
A series of β-diketonate, keto(aryl)iminato, and β-bis(aryl)iminato complexes of difluoroboron, twenty in total, have been prepared to assess the impact of chelate ring and aniline substitution on the structural, electrochemical, and photophysical properties of these ubiquitous chelates. DFT (B3LYP/6-31G*) calculations supplemented the experimental results and both demonstrated that replacing oxygen with the more electron-donating aniline groups serves to only fine-tune the electronic properties because both the HOMO and LUMO energies are affected by such substitution. The electronic properties of all compounds are most greatly influenced by the nature of the substituents bound to the carbon portion of the chelate ring. …
Atr-Ftir Spectroscopic Analysis Of Sorption Of Aqueous Analytes Into Polymer Coatings Used With Guided Sh-Saw Sensors, Yolanda K. Jones, Zhonghui Li, Michael M. Johnson, Fabien Josse, Jeanne Hossenlopp
Atr-Ftir Spectroscopic Analysis Of Sorption Of Aqueous Analytes Into Polymer Coatings Used With Guided Sh-Saw Sensors, Yolanda K. Jones, Zhonghui Li, Michael M. Johnson, Fabien Josse, Jeanne Hossenlopp
Chemistry Faculty Research and Publications
Attenuated total internal reflectance Fourier transform infrared (ATR-FTIR) spectroscopy was used for the investigation of sorption of aqueous solutions of analytes into polymer coatings. A series of simple model polymers, such as poly(dimethylsiloxane), poly(epichlorhydrin), and poly(isobutylene), and films and analytes, such as aqueous solutions of ethylbenzene, xylenes, toluene, and nitrobenzene, were used to evaluate the use of ATR-FTIR spectroscopy as a screening tool for sensor development. The ratios of integrated infrared absorption bands provided a simple and efficient method for predicting trends in partition coefficients. Responses of polymer-coated guided shear horizontal surface acoustic wave (SH-SAW) sensor platforms to the series …