The proximity of anthryl groups is an important factor governing opto-electronic and film properties of anthracene containing polymers used in technological applications. The surface mechanical properties of a series of poly(methyl methacrylate-co-9-anthryl methyl methacrylate) are described. Th...
The quantum yields of fluorescence and photoisomerization of trans-1-(9-anthryl)-2-(n-pyridyl)ethenes (n = 2, 3 or 4) (tn-ApyE) and the corresponding cis isomers (n = 2 or 4) (c-n-APyE) were measured in various solvents. t-3-APyE is strongly fluorescent, but does not undergo photoisomerization, ...
A mixture of the E and Z isomers of ethyl 2-cyano-3-((4-fluorophenyl)amino) acrylate was synthesized and characterized by elemental analysis, attenuated total reflectance-Fourier transform infrared spectroscopy, 1H and 13C nuclear magnetic resonance spectroscopy. The structure of the Z isomer wa...
Caffeic acid phenethyl ester (CAPE) has recently been shown to potently stimulate glucose uptake in cultured skeletal muscle cells through the AMPK pathway and therefore to have anti-diabetic potential. We report here that CAPE increases glucose uptake in C2C12 muscle cells by 225 ± 21% at 50 μ...
The NNW-SSE trending Mariánské Lázně Fault (MLF) zone is situated in the western part of the Bohemian Massif (Czech Republic, central Europe) and controls the eastern limit of Cenozoic Cheb Basin. The Cheb Basin is well-known for present-day earthquake swarms, with maximum magnitude not exce...
Equilibrative nucleoside transporters (ENTs) play a crucial role in the transport of nucleoside and nucleoside analogues, which are important for nucleotide synthesis and chemotherapy. In addition, ENTs regulate extracellular adenosine levels in the vicinity of its receptors and hence influence ...
This paper describes the synthesis of N-pyridinyl(alkyl)phthalimides related to N-phenyl-4,5,6,7-tetrafluorophthalimides known to be inhibitors of tumour necrosis factor-α (TNFα) production. Pharmacomodulation at the phthalimidic nitrogen led to the selection of two pharmacophoric fragments (2...
Activating mutations in the BRAF serine/threonine kinase are found in more than 70% of human melanomas, >90% of which are BRAFV600E. It provides new therapeutic opportunities in malignant melanoma. In silico and in vitro screening of our compound collection has identified Hit 2 as BRAFV600E inhi...
Sourdough is a low-pH, fermented product prepared using lactic acid bacteria and yeast mixed with rye flour, wheat flour, and water. It is used and backslopped in bakeries because it enhances texture, flavor, and dough expansion of bread. Various lactic acid bacteria and yeasts have been identif...
In the present study, we have synthesized some novel 4-(4-(2-isonicotinoylhydrazinyl)-6-((aryl)amino)-1,3,5-triazin-2-ylamino)-N-(pyrimidin-2-yl)benzenesulfonamide derivatives (3a–v) and evaluated their in vitro antimicrobial activity against the representative panel of Gram-positive bacteria [...
Kinase irregularity has been correlated with several complex neurodegenerative tauopathies. Development of selective inhibitors of these kinases might afford promising anti-tauopathy therapies. While DAPK1 inhibitors halt the formation of tau aggregates and counteract neuronal death, CSF1R inhib...
We describe a kinetic study by differential scanning calorimetry (DSC) of the thermal decomposition under a nitrogen atmosphere of several adducts with pyridine or substituted pyridines of bis(5,7-dichloro-8-quinolinol)oxovanadium(IV), to which the formula assigned is VO(clox)2· B, where clox =...
An efficient process for the reductive cleavage of NO bonds using samarium diiodide is detailed for a variety of structural types to define the scope and limitations of the method. The reduction is shown to be compatible with base sensitive substrates such as trifluoroacetamide derivatives, wh...
α-Chymotrypsin (CT) is slowly inhibited by N-nitroso-N-benzylacetamide (1) at 25°C. The 13C-NMR spectrum of the hydrolysate of 13C-enriched 1-inhibited CT shows five new signals at 52.33, 44.55, 43.72, 36.79, and 32.90 ppm resulting from alkylation of the side chains and also of amide linkages...
Axially chiral 5,5-dimethyl-3-(o-aryl)rhodanine, 3-(o-aryl)rhodanine and 5,5-dimethyl-3-(o-aryl)-2-thioxo-4-oxazolidinone derivatives have been synthesized as racemates and the energy barriers to enantiomerization have been determined by dynamic 1H NMR or by following the thermal equilibration o...
Alkylation and aldol reactions carried out on axially chiral, diastereoenriched oxazolidinedione derivatives were found to be highly stereoselective with respect to substitution at the 5-position of the oxazolidindione ring. Thus, diastereoenriched 5-methyl-3-(o-iodophenyl)-2-thioxo-4-oxazolidin...
BackgroundOxazolidinones derivatives exhibit different biological properties, including anticancer activity. This work aimed to investigate the anticancer potential of five novel 2-Thioxo-oxazolidin-4-one derivatives.
Future fuels will be developed from a variety of biomass and fossil sources, and this presents an opportunity to design new fuels that carry a much reduced environmental burden. To this end, understanding how the molecular structure of a fuel impacts on the processes of combustion and emissions ...
The activity and selectivity of silica-supported Hoveyda–Grubbs (HG) complex for the cross-metathesis of methyl oleate with 1-hexene to obtain 1-decene, methyl 9-tetradecenoate, 5-tetradecene and methyl 9-decenoate were studied in a batch reactor. The HG complex loading was varied between 0.87 ...
A series of higher 2-alkenes, i.e., 2-pentene, 2-hexene and 2-octene were polymerized with phenyl substituted α-diimine nickel complexes in combination with modified methylaluminoxane (MMAO) to produce branched poly(2-alkene)s with high molecular weight and narrow molecular weight distribution ...
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