Filtry
wszystkich: 908
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Wyniki wyszukiwania dla: CARNOSINE DERIVATIVES
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Synthesis and SAR Studies of Antibacterial Peptidyl Derivatives Based upon the Binding Site of Human Cystatin C
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Sonochemical synthesis of rosuvastatin based novel 3-methyleneisoindolin-1-one derivatives as potential anticancer agents
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High yield synthesis and preliminary spectroscopic study of mono-N-alkylated cyclen derivatives of salicylic acid
PublikacjaW artykule przedstawiono reakcję bezpośredniego alkilowania cyklenu bromopochodnymi kwasu salicylowego. Otrzymane związki wykorzystano do badań spektroskopowych. Stwierdzono, że tworzą one wybiórczo kompleksy z jonami metali grupy II. Wyznaczono stałe tworzących się kompleksów.
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Analysis of bisphenols and their derivatives in infant and toddler ready-to-feed milk and powdered milk by LC MS/MS
PublikacjaReady-to-feed milk and powdered milk packed in different types of packaging lined with resin are chosen as the primary or complementary diet for infants and toddlers. An HPLC–MS/MS method was established and validated for the determination of nineteen bisphenols and their derivatives in such samples. The recoveries were from 31% to 120%, while the values of limit of detection and quantification were in the range of 0.24–0.40 and...
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The Synthesis of 3-Amino-pyrazine-2-carbohydrazide and 3-Amino-N'-methylpyrazine-2-carbohydrazide Derivatives
PublikacjaW poszukiwaniu biologicznie aktywnych związków otrzymano szereg pochodnych 3-Amino-pirazyno-2-karbohydrazydu i 3-Amino-N'-metylopirazyno-2-karbohydrazydu w wyniku reakcji hydrazydu aminopirazynoinowegokwasu z izocyjanianami, aldehydami, ketonami, CS2 i kwasem mrówkowym.
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Assessing ecotoxicity and the endocrine potential of selected phthalates, BADGE and BFDGE derivatives in relation to environmentally detectable levels
PublikacjaThere is no doubt that the subject area of plasticmaterials (e.g., production of epoxy resins or polyesters) is inherently connected to issues concerning bisphenol A (BPA) and its analogues. Unfortunately, much less attention has been given to other compounds, which are also used for the production of these materials. Bisphenol A diglycidyl ether (BADGE) is a synthetic industrial compound obtained by a condensation reaction between...
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Effect of temperature and ionic strength on volumetric and acoustic properties of solutions of urea alkil derivatives in aqueous NaCl
PublikacjaThe present work was undertaken to study volumetric and acoustic properties for diluted solutions of tetramethylurea in pure water and for urea, n-propylurea, n-butylurea and tetramethylurea in 0.5 or 1 moldm3 aqueous solutions of sodium chloride. This paper presents measured values of densities and sound velocities at T = (288.15, 298.15 and 308.15) K. From these data the apparent molar volumes, , adiabatic compressibilities,...
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Synthesis and biological evaluation of fluorinated 3-phenylcoumarin-7-O-sulfamate derivatives as steroid sulfatase inhibitors
PublikacjaIn the present work, we report the initial results of our study on a series of 3-phenylcoumarin sulfamate-based compounds containing C-F bonds as a novel inhibitors of steroid sulfatase (STS). The new compounds are potent STS inhibitors, possessing more than 10 times higher inhibitory potency than coumarin-7-O-sulfamate. In the course of our investigation, compounds 2b and 2c demonstrated the highest inhibitory effect in the enzymatic...
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Extracting functional groups of ALLINI to design derivatives of FDA‐approved drugs: Inhibition of HIV‐1 integrase
PublikacjaHIV‐1 integrase (IN) is crucial for integration of viral DNA into the host genome and a promising target in development of antiretroviral inhibitors. In this work, six new compounds were designed by linking the structures of two different class of HIV‐1 IN inhibitors (active site binders and allosteric IN inhibitors (ALLINIs)). Among newly designed compounds, INRAT10b was found most potent HIV‐1 IN inhibitor considering different...
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Chloroacridine derivatives as potential anticancer agents which may act as tricarboxylic acid cycle enzyme inhibitors
PublikacjaThe chloroacridines affect biological forms of melanoma in different ways. Amelanotic (Ab) melanoma (with inhibited melanogenesis and higher malignancy) was particularly sensitive to the action of the chloroacridines. The Ab melanoma cells died through apoptosis and through death without caspase activation. Diminished activity of TAC enzymes was noticed among Ab melanoma cells together with ATP/NAD depletion, especially in the...
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5-Selenocyanato and 5-trifluoromethanesulfonyl derivatives of 2′-deoxyuridine: synthesis, radiation and computational chemistry as well as cytotoxicity
Publikacja5-Selenocyanato-2′-deoxyuridine (SeCNdU) and 5-trifluoromethanesulfonyl-2′-deoxyuridine (OTfdU) have been synthesized and their structures have been confirmed with NMR and MS methods. Both compounds undergo dissociative electron attachment (DEA) when irradiated with X-rays in an aqueous solution containing a hydroxyl radical scavenger. The DEA yield of SeCNdU significantly exceeds that of 5-bromo-2′-deoxyuridine (BrdU), remaining...
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Exploring the Reactivity of Unsymmetrical Diphosphanes toward Heterocumulenes: Access to Phosphanyl and Phosphoryl Derivatives of Amides, Imines, and Iminoamides
PublikacjaWe present a comprehensive study on the diphosphanation of iso(thio)cyanates by unsymmetrical diphosphanes. The reactions involving unsymmetrical diphosphanes and phenyl isocyanate or phenyl thioisocyanate gave rise to phosphanyl, phosphoryl, and thiophosphoryl derivatives of amides, imines, and iminoamides. The structures of the diphosphanation products were confirmed through NMR spectroscopy, IR spectroscopy, and single-crystal...
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Analysis of the influence of polystyrene microplastics and their derivatives on the DNA of human colon epithelial cells HT29 with the comet assay
PublikacjaWe have been using plastic for almost a century and nowadays a lot of them circulates as pollutants in the environment and still defragmenting to micro and nanoscale. The exposition through the food chain and its precise impact on human health is still not clear. In our study, we tested real food packaging after contact with food products and real thermoinsulation and environmental samples of polystyrene in different model liquids,...
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Palindromic carbazole derivatives: unveiling their antiproliferative effect via topoisomerase II catalytic inhibition and apoptosis induction
PublikacjaHuman DNA topoisomerases are essential for crucial cellular processes, including DNA replication, transcription, chromatin condensation, and maintenance of its structure. One of the significant strategies employed in cancer treatment involves the inhibition of a specific type of topoisomerase, known as topoisomerase II (Topo II). Carbazole derivatives, recognised for their varied biological activities, have recently become a significant...
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CYP3A4 overexpressin enhances the cytotoxicity of the antitumor triazoloacridinone derivative C-1305 in CHO cells
PublikacjaW pracy badano wpływ nadekspresji izoenzymu CYP3A4 na cytotoksyczność i odpowiedź komórkową indukowaną przez przeciwnowotworową pochodną triazoloakrydonu w modelowym układzie komórek CHO: dzikego typu, z nadekspresją reduktazy cytochromu P450 (CHO-HR) oraz z koekspresją reduktazy i izoenzymu CYP3A4 (CHO-HR-3A4). Wykazano, że komórki CHO wykazywały różną wrażliwość na badany związek, a linia CHO-HR okazała się najbardziej wrażliwa,...
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CYP3A4 overexpression enhances the cytotoxicity of the antitumor triazoloacridinone derivative C-1305 in CHO cells
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In vitro photodynamic activity of lipid vesicles with zinc phthalocyanine derivative against Enterococcus faecalis
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Polymeric bisphosphonate derivative of ciprofloxacin – synthesis, structural analysis and antibacterial activity of the prospective conjugate
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Initial value problems for neutral fractional differential equations involving a Riemann-Liouville derivative
PublikacjaBadano równania neutralne typu ułamkowego z odchylonym argumentem. Podano warunki dostateczne na istnienie jednego rozwiązania.
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Thermodynamic, Anticoagulant, and Antiproliferative Properties of Thrombin Binding Aptamer Containing Novel UNA Derivative
PublikacjaThrombin is a serine protease that plays a crucial role in hemostasis, fibrinolysis, cell proliferation, and migration. Thrombin binding aptamer (TBA) is able to inhibit the activity of thrombin molecule via binding to its exosite I. This 15-nt DNA oligonucleotide forms an intramolecular, antiparallel G-quadruplex structure with a chair-like conformation. In this paper, we report on our investigations on the influence of certain...
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Solvent-Free Synthesis of Phosphonic Graphene Derivative and Its Application in Mercury Ions Adsorption
PublikacjaFunctionalized graphene was efficiently prepared through ball-milling of graphite in the presence of dry ice. In this way, oxygen functional groups were introduced into material. The material was further chemically functionalized to produce graphene derivative with phosphonic groups. The obtained materials were characterized by spectroscopic and microscopic methods, along with thermogravimetric analysis. The newly developed material...
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Induction of apoptosis by triazoloacridinone derivative - C-1533 in HL60 and MOLT4 human leukemia cells.
PublikacjaPrzeprowadzone badania miały na celu określenie zdolności triazoloakrydonu C-1533 do indukcji śmierci komórek nowotworowych MOLT4 i HL60 na drodze apoptozy. Badanie zjawiska apoptozy przeprowadzono z wykorzystaniem techniki cytofluorymetrii przepływowej, mikroskopii fluorescencyjnej i elektroforezy agarozowej. Badania wykazały, że zarówno w komórkach MOLT4 jak i HL60, spadek mitochondrialnego potencjału błonowego oraz translokacja...
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On the Fenchel–Moreau conjugate of G-function and the second derivative of the modular in anisotropic Orlicz spaces
PublikacjaIn this paper, we investigate the properties of the Fenchel–Moreau conjugate of G-function with respect to the coupling function c(x, A) = |A[x]2 |. We provide conditions that guarantee that the conjugate is also a G-function. We also show that if a G-function G is twice differentiable and its second derivative belongs to the Orlicz space generated by the Fenchel–Moreau conjugate of G then the modular generated by G is twice differentiable...
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Time fractional analysis of Casson fluid with application of novel hybrid fractional derivative operator
PublikacjaA new approach is used to investigate the analytical solutions of the mathematical fractional Casson fluid model that is described by the Constant Proportional Caputo fractional operator having non-local and singular kernel near an infinitely vertical plate. The phenomenon has been expressed in terms of partial differential equations, and the governing equations were then transformed in non-dimensional form. For the sake of generalized...
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Synthesis of new antrapyridazone derivatives - a novel group of anticancer agents active on a multidrugresistant(MDR) tumor cell lines
PublikacjaNovel antrapyridazone derivatives were synthesized and biologically evaluated in order tobroaden the data on structure-activity relationship of this class of cytostatics. Recent literaturedata prove that acetamides react better with aryl chlorides. A new approach based onintroduction of other amides form into aromatic ring in Ullmann was tested. This new methodcould give better yields and make purification step more convenient.
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Preliminary Microbiological Tests of S-Carvone and Geraniol and Selected Derivatives of These Compounds That May Be Formed in the Processes of Isomerization and Oxidation
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Adsorption of Hydrocarbon Chloro-Derivatives onto DTO Commercial Activated Carbon from Multi-Component Aqueous Solutions
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N-Substituted piperazine derivatives as potential multitarget agents acting on histamine H3 receptor and cancer resistance proteins
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Crystallographic studies of piperazine derivatives of 3-methyl-5-spirofluorenehydantoin in search of structural features of P-gp inhibitors
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Density Functional Theory Studies on Ir Spectra of the Triphenylene Derivatives. A Scaled Quantum Mechanical Force Field Approach
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Anti-Helicobacter pylori activities of selected N-substituted cinnamamide derivatives evaluated on reference and clinical bacterial strains
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Photophysical properties of 3-[2-(N-phenylcarbazolyl)benzoxazol-5-yl]alanine derivatives – experimental and theoretical studies
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Metabolism of antitumor 9-amino-1-nitroacridine derivatives in HepG2 cells and its influence on cytochrome P450 isoenzymes
PublikacjaCelem przeprowadzonych badań było określenie wpływu pochodnych C-857 i C-1748 na poziom enzymów cytochromu P450 w powiązaniu z kinetyką metabolizmu badanych związków. Eksperymenty zostały przeprowadzone na komórkach ludzkiego nowotworu wątroby HepG2. Uzyskane wyniki metodą Western blotting wykazały, że za metaboliczną transformacje pochodnych C-857 i C-1748 odpowiada izoenzym CYP3A4.Analiza metabolitów (Western blotting, HPLC)...
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O-substituted tetrahydroxamate derivatives of p-tert-butylcalix[4]arene as receptors for transition and heavy metal cations
PublikacjaTetrasubstituted O-hydroxamate derivatives of p-tert-butylcalix[4]arene were applied as active materials in ion-selective membrane electrodes and were tested towards Pb-selectivity. The electrodes gave near-Nernstian characteristics for Pb2+ cations. The selectivity coefficients were determined. The influence of plasticizer on the electrode behaviour was studied. The dependence of the chemical structure on selectivity coefficients...
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Nanoconjugates of graphene oxide derivatives and meso-tetraphenylporphyrin: a new avenue for anticancer photodynamic therapies – Cell-on-a-Chip analysis
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Advantages and limitations of classic and 3D QSAR approaches in nano-QSAR studies based on biological activity of fullerene derivatives
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Potential of Waste Biomass from the Sugar Industry as a Source of Furfural and Its Derivatives for Use as Fuel Additives in Poland
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Qualitative analysis of phospholipids and their oxidised derivatives – used techniques and examples of their applications related to lipidomic research and food analysis
PublikacjaPhospholipids (PLs) are important biomolecules that not only constitute structural building blocks and scaffolds of cell and organelle membranes, but also play a vital role in cell biochemistry and physiology. Moreover, dietary exogenous PLs are characterized by high nutritional value and other beneficial health effects, which are confirmed by numerous epidemiological studies. For this reason, PLs are of high interest in lipidomics...
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Efficient Gradient-Based Algorithm with Numerical Derivatives for Expedited Optimization of Multi-Parameter Miniaturized Impedance Matching Transformers
PublikacjaFull-wave electromagnetic (EM) simulation tools have become ubiquitous in the design of microwave components. In some cases, e.g., miniaturized microstrip components, EM analysis is mandatory due to considera¬ble cross-coupling effects that cannot be accounted for otherwise (e.g., by means of equivalent circuits). These effects are particularly pronounced in the structures in¬volving slow-wave compact cells and their numerical...
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Diphosphination of CO2 and CS2 mediated by frustrated Lewis pairs - catalytic route to phosphanyl derivatives of formic and dithioformic acid
PublikacjaThe first example of CO2 diphosphination is described. Reactions of unsymmetrical diphosphanes with CE2 (E = O, S) catalyzed by BPh3 insert a CE2 molecule into the P-P bond with formation of the products of the general formula R2P-E-C(=E)-PR2. The obtained CO2 adducts arise from synergistic interaction of diphosphane and borane with CO2 molecule.
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Meldrum’s acid assisted formation of tetrahydroquinolin‑2‑one derivatives a short synthetic pathway to the biologically useful scaffold
PublikacjaA new method for the preparation of tetrahydroquinolin-2-one derivatives is presented. This approach involves a two-step reaction between enaminones and acylating agents, immediately followed by electrophilic cyclization, all within a single synthesis procedure, eliminating the need to isolate intermediates. The entire process is facilitated by the use of acyl Meldrum’s acids which not only shortens the preparation time of the...
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Human carnosinases: A brief history, medicinal relevance, and in silico analyses
PublikacjaCarnosine, an endogenous dipeptide, has been found to have a plethora of medicinal properties, such as antioxidant, antiageing, and chelating effects, but with one downside: a short half-life. Carnosinases and two hydrolytic enzymes, which remain enigmatic, are responsible for these features. Hence, here we emphasize why research is valuable for better understanding crucial concepts like ageing, neurodegradation, and cancerogenesis,...
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Synthesis, characterization, and electrochemical testing of carbon nanotubes derivatized with azobenzene and anthraquinone.
PublikacjaWielościenne i jednościenne nanorurki węglowe modyfikowano na ścianach bocznych związkami elektrochemicznie aktywnymi, takimi jak azobenzen i antrachinon. Funkcjonalizowane nanorurki badano technikami spektroskopowymi i elektrochemicznymi oraz wykorzystując mikroskopię elektronową. Wyniki tych badań potwierdziły chemiczną modyfikację.
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Transport of lead across polymer inclusion membrane with p-tert-butylkalix[4]arene derivative
PublikacjaOpisane zostały ułatwienia w transporcie jonów ołowiu (II) przez polimerową membranę inkluzyjną (PIMs),która składała się z trój octanu celulozy jako polimerowego suportu, eteru o-nitrofenylooktylu jako plastyfikatora i 25,26,27,28, tetra-(N-hydroksy-N-metylokarbonylo metoksy)-p-tert-butylokaliks[4]arenu jako nośnika jonów. Polimerowa membrana inkluzyjna została scharakteryzowana przy pomocy mikroskopu sił atomowych (AFM). Otrzymane...
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Enzymatically catalyzed furan-based copolyesters containing dimerized fatty acid derivative as a building block
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Numerical and quantitative analysis of HIV/AIDS model with modified Atangana-Baleanu in Caputo sense derivative
PublikacjaFractional calculus plays an important role in the development of control strategies, the study of the dynamical transmission of diseases, and some other real-life problems nowadays. The time-fractional HIV/AIDS model is examined using a novel method in this paper. Based on the Atangana-concept Baleanu’s of a derivative in the Caputo sense, the current modified fractional derivative operator uses singular and non-local kernels....
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Antitumor 1-nitroacridine derivative C-1748 induces significant apoptosis in pancreatic cancer cells.
PublikacjaPancreatic cancer is the fifth leading cause of cancer death and has the lowest survival rate of any solid cancer in the industrial countries. The poor prognosis of pancreatic cancer results from its tendency for late presentation, aggressive invasion, early metastasis, and resistance to chemotherapy. Gemcitabine still remains the best chemotherapeutic agent available for the treatment of advanced pancreatic cancer. However, gemcitabine...
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Metabolism of antitumour agent 1-nitroacridine derivative, C-1748 in pancreatic cancer cell lines
PublikacjaPancreatic cancer has the highest mortality rate of all major cancers because of limited treatment options. Surgical removal of the tumour is possible only in its early stage, nevertheless the asymptomatic development very often makes unable an accurate diagnose. In the case of metastatic pancreatic cancer only chemotherapy, mainly with gemcitabine, can be offered to patients. However, common resistance towards gemcitabine imposes...
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Photosensitive and pH-dependent activity of pyrazine-functionalized carbazole derivative as promising antifungal and imaging agent
PublikacjaCarbazole skeleton plays a significant role as a structural scaffold of many pharmacologically active compounds. Pyrazine-functionalized carbazole derivative was constructed by coupling 2-amino-5-bromo-3-methylaminepyrazine (ABMAP) into 3 and 6 positions of the carbazole ring. Multi-experimental methods were used, e.g., potentiometric, spectroscopic (ATR, UV, XRD powder,1H and13C NMR), electrochemical (cyclic voltammetry), and...
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Interactions of amphotericin B derivative of low toxicity with biological membrane components - the Langmuir monolayer approach
PublikacjaMetodą monowarstw Langmuira zbadano naturę oddziaływań nowej pochodnej antybiotyku przeciwgrzybowego amfoterycyny B o niskiej toksyczności, tj. estru metylowego N-metylo-N-D-fruktopiranozyloamfoterycyny B (MF-AME)z komponentami błon biologicznych: ergosterolem, występującym w komórkach grzybowych i cholesterolem występującym w komórkach zwierzęcych oraz z modelowym fosfolipidem DPPC i na tej podstawie stwierdzono, że zróżnicowanie...