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311.
Design,Synthesis, and Evaluation of an 18F‐Labeled Radiotracer Based on Celecoxib–NBD for Positron Emission Tomography (PET) Imaging of Cyclooxygenase‐2 (COX‐2) 下载免费PDF全文
Dr. Jatinder Kaur Ole Tietz Dr. Atul Bhardwaj Alison Marshall Jenilee Way Dr. Melinda Wuest Prof. Frank Wuest 《ChemMedChem》2015,10(10):1635-1640
A series of novel fluorine‐containing cyclooxygenase‐2 (COX‐2) inhibitors was designed and synthesized based on the previously reported fluorescent COX‐2 imaging agent celecoxib–NBD ( 3 ; NBD=7‐nitrobenzofurazan). In vitro COX‐1/COX‐2 inhibitory data show that N‐(4‐fluorobenzyl)‐4‐(5‐p‐tolyl‐3‐trifluoromethylpyrazol‐1‐yl)benzenesulfonamide ( 5 ; IC50=0.36 μM , SI>277) and N‐fluoromethyl‐4‐(5‐p‐tolyl‐3‐trifluoromethylpyrazol‐1‐yl)benzenesulfonamide ( 6 ; IC50=0.24 μM , SI>416) are potent and selective COX‐2 inhibitors. Compound 5 was selected for radiolabeling with the short‐lived positron emitter fluorine‐18 (18F) and evaluated as a positron emission tomography (PET) imaging agent. Radiotracer [18F] 5 was analyzed in vitro and in vivo using human colorectal cancer model HCA‐7. Although radiotracer uptake into COX‐2‐expressing HCA‐7 cells was high, no evidence for COX‐2‐specific binding was found. Radiotracer uptake into HCA‐7 tumors in vivo was low and similar to that of muscle, used as reference tissue. 相似文献
312.
313.
This study reports copolymer composition tailored wrapping of carbon nanotubes, leading to a gigantic dielectric permittivity and peculiar nonlinear rheological response in a nonfluoro copolymer/carbon nanotube (CNT) hybrid system. Specifically, we observed a strong interfacial polarization effect in ethylene vinyl acetate (EVAc) copolymer/CNT nanocomposites, resulting in a dielectric permittivity of approximately 4000 at 10 Hz and 450 (dielectric loss <1) at 1 kHz, with only 1% volume fraction of CNTs and 40% vinyl acetate (VAc) content. No such effect was observed in EVAc with 12% VAc. Extensive amplitude oscillatory rheology studies prompted us to propose a novel hook-wrap-type mechanism, wherein polar interactions act as hooks and nonpolar segments allow wrapping, depending on the optimal interactions between the CNT and copolymer. Raman spectroscopy, small-angle x-ray scattering, and relaxation studies also revealed a significant change in segmental dynamics and mass fractal compactness with a change in the VAc content. This work provides a melt processing-based scalable route to develop polymer dielectrics while advancing the fundamental understanding of polymer-CNT interactions and the underlying mechanisms of dielectric behavior in nanocomposites. 相似文献
314.
Saurabh Bhardwaj 《Numerical Heat Transfer, Part A: Applications》2013,63(9):972-991
In the present study, natural convection in a two-dimensional porous right-angled triangular enclosure with one wavy wall is studied numerically. Three cases with one, two, and three undulations on the left wall are studied in this analysis. The stream function-vorticity equations are solved using finite-difference technique and a structured nonorthogonal body-fitted mesh is used for computations. The effect of Rayleigh number (Ra = 103–106), Darcy number (Da = 10?4–10?2) and undulations on the heat transfer, fluid flow, and entropy generation is investigated. It is found that average Nusselt number increases with Darcy number and number of undulations present on the left wall at fixed Darcy number. 相似文献
315.
Shashi B. Rana Vimal K. Bhardwaj Satbir Singh Amarpal Singh Navneet Kaur 《Journal of Experimental Nanoscience》2014,9(9):877-891
In this study, a precipitation method was used to synthesise ZnO nanoparticles using suitable precursors. An efficient surface modification method was proposed in order to reduce the agglomeration among synthesised small sized ZnO nanoparticles using 2-aminothiophenol as a capping agent. This article briefly investigated the effects of capping agent like 2-aminothiophenol on the optoelectronic properties of ZnO nanoparticles. The modified effectivity of 2-aminothiophenol has been examined on the nanosized ZnO nanoparticle for fluorescence and UV–visible (UV–vis) studies. The mechanism was studied for ZnO nanoparticles light emitting capability under different conditions. By facilitating the capping of ZnO with 2-aminothiophenol, fluorescence emission of the surface defects vanishes and ultraviolet (UV) emission increases. Surface capping by 2-aminothiophenol effectively covers most of the surface defects of ZnO and results in quenching of the visible region. The UV–vis absorption spectra of modified ZnO nanoparticles has been influenced by modified ZnO nanoparticles as a result of surface modification; where marked blue shift in absorption edge results. By surface modification of ZnO nanoparticles, change in optoelectronics properties has opened the new scope and possibilities to explore and fine tune the optical character of the modified ZnO for various optoelectronics applications such as UV laser. 相似文献
316.
K. A. Dubey Y. K. Bhardwaj Lata Panicker C. V. Chaudhari Virendra Kumar N. K. Goel S. Sabharwal 《应用聚合物科学杂志》2008,110(6):3552-3559
The miscibility of polychloroprene rubber (CR) and ethylene–propylene–diene terpolymer rubber (EPDM) was studied over the entire composition range. Different blend compositions of CR and EPDM were prepared by initially mixing on a two‐roll mill and subsequently irradiating to different gamma radiation doses. The blends were characterized by differential scanning calorimetry, Fourier transform infrared spectroscopy, density measurement, hardness measurement, and solvent permeability analysis. The compatibility of the blends was studied by measuring the glass transition temperature and heat capacity change of the blends. The immiscibility of blends was reflected by the presence of two glass transition temperatures; however, partial miscible domains were observed due to inter diffusion of phases. Permeation data fitted best with the Maxwell's model and indicated that in CR‐EPDM blends, EPDM exists as continuous phase with CR as dispersed phase for lower CR weight fractions and phase inversion occurred in 40–60% CR region. It was observed that CR improved oil resistance of EPDM; however, the effect was prominent for blends of >20% CR content. © 2008 Wiley Periodicals, Inc. J Appl Polym Sci, 2008 相似文献