Search results for: CARNOSINE DERIVATIVES
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Fourier transform infrared spectroscopic and theoretical study of water interactions with glycine and its N-methylated derivatives
PublicationZbadano hydratację glicyny i jej metylowych pochodnych: N-metyloglicyny (NMG), N,N-dimetyloglicyny (DMG) i N,N,N-trimetyloglicyny (TMG) przy wykorzystaniu spektroskopii FTIR, z zastosowaniem cząsteczki HDO jako sondy molekularnej. Ilościowa wersja metody widm różnicowych pozwoliła na wyizolowanie widma wody zaburzonej przez substancję rozpuszczoną. Wyniki widmowe zostały skonfrontowane z obliczeniami teoretycznymi w ramach teorii...
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The antitumor derivatives, C1305 and C1748, were different in effects on CYP3A4 expression and catalytic activity in HepG2 cells
PublicationCytochromy P450 (CYP) należą do grupy enzymów biorących udział w 70-80% metabolizmu fazy I większości stosowanych klinicznie leków. Z tego powodu oddziaływanie leków z enzymami cytochromu P450 stało się istotnym elementem w projektowaniu chemoterapeutyków, szczególnie tych, które są stosowane w terapii wielolekowej. Znajomość substratów, induktorów i inhibitorów poszczególnych izoenzymów P450, nie tylko może obniżać częstość występowania...
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The Synthesis of 3-Amino-pyrazine-2-carbohydrazide and 3-Amino-N'-methylpyrazine-2-carbohydrazide Derivatives
PublicationW 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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Application of the PASSIL technique for the passive sampling of exemplary polar contaminants (pharmaceuticals and phenolic derivatives) from water
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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
PublicationW 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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Synthesis and Thermal, Photophysical, Electrochemical Properties of 3,3-di[3-Arylcarbazol-9-ylmethyl]oxetane Derivatives
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Exploring Alkyl Ester Salts of L-Amino Acid Derivatives of Ibuprofen: Physicochemical Characterization and Transdermal Potential
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Phthalocyanine Derivatives Possessing 2-(Morpholin-4-yl)ethoxy Groups As Potential Agents for Photodynamic Therapy
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Search for new tools to combat Gram-negative resistant bacteria among amine derivatives of 5-arylidenehydantoin
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Solid phase synthesis of 4,5,8-trihydroxy-9,10-anthraquinone-1-yl-(tuftsin or retro-tuftsin) derivatives
PublicationPrzedstawiono syntezę na fazie stałej połączeń leuko-1,4,5,8-tetra-hydroksyantrachinonów z pochodnymi tuftsyny i retro-tuftsyny zawierającymi wiązanie izopeptydowe. Do syntezy wykorzystano standardową metodę Fmoc i DIC jako odczynnik aktywujący.
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Chloroacridine derivatives as potential anticancer agents which may act as tricarboxylic acid cycle enzyme inhibitors
PublicationThe 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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Palindromic carbazole derivatives: unveiling their antiproliferative effect via topoisomerase II catalytic inhibition and apoptosis induction
PublicationHuman 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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Analysis of bisphenols and their derivatives in infant and toddler ready-to-feed milk and powdered milk by LC MS/MS
PublicationReady-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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Exploring the Reactivity of Unsymmetrical Diphosphanes toward Heterocumulenes: Access to Phosphanyl and Phosphoryl Derivatives of Amides, Imines, and Iminoamides
PublicationWe 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
PublicationWe 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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Assessing ecotoxicity and the endocrine potential of selected phthalates, BADGE and BFDGE derivatives in relation to environmentally detectable levels
PublicationThere 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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5-Selenocyanato and 5-trifluoromethanesulfonyl derivatives of 2′-deoxyuridine: synthesis, radiation and computational chemistry as well as cytotoxicity
Publication5-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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Extracting functional groups of ALLINI to design derivatives of FDA‐approved drugs: Inhibition of HIV‐1 integrase
PublicationHIV‐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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Effect of temperature and ionic strength on volumetric and acoustic properties of solutions of urea alkil derivatives in aqueous NaCl
PublicationThe 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
PublicationIn 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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CYP3A4 overexpression enhances the cytotoxicity of the antitumor triazoloacridinone derivative C-1305 in CHO cells
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Initial value problems for neutral fractional differential equations involving a Riemann-Liouville derivative
PublicationBadano równania neutralne typu ułamkowego z odchylonym argumentem. Podano warunki dostateczne na istnienie jednego rozwiązania.
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CYP3A4 overexpressin enhances the cytotoxicity of the antitumor triazoloacridinone derivative C-1305 in CHO cells
PublicationW 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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Polymeric bisphosphonate derivative of ciprofloxacin – synthesis, structural analysis and antibacterial activity of the prospective conjugate
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In vitro photodynamic activity of lipid vesicles with zinc phthalocyanine derivative against Enterococcus faecalis
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On the Fenchel–Moreau conjugate of G-function and the second derivative of the modular in anisotropic Orlicz spaces
PublicationIn 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
PublicationA 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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Thermodynamic, Anticoagulant, and Antiproliferative Properties of Thrombin Binding Aptamer Containing Novel UNA Derivative
PublicationThrombin 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
PublicationFunctionalized 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.
PublicationPrzeprowadzone 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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Cytotoxicity of anthraquinone derivatives (Compound 1-9) towards H226 cancer cell
Open Research DataThis study presents absorbance values of formazan product (converted from MTT) which corresponds to the cytotoxicity of anthraquinone derivatives (Compound 1-9) towards H226 cancer cells.
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Cytotoxicity of anthraquinone derivatives (Compound 1-9) towards A549 cancer cells
Open Research DataThis study presents absorbance values of formazan product (converted from MTT) which corresponds to the cytotoxicity of anthraquinone derivatives (Compound 1-9) towards A549 cancer cells.
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Cytotoxicity of anthraquinone derivatives (Compound 1-9) towards NHBE normal cells
Open Research DataThis study presents absorbance values of formazan product (converted from MTT) which corresponds to the cytotoxicity of anthraquinone derivatives (Compound 1-9) towards NHBE normal cells.
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Cytotoxicity of anthraquinone derivatives (Compound 1-9) towards H460 cancer cell
Open Research DataThis study presents absorbance values of formazan product (converted from MTT) which corresponds to the cytotoxicity of anthraquinone derivatives (Compound 1-9) towards H460 cancer cells.
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Synthesis of new antrapyridazone derivatives - a novel group of anticancer agents active on a multidrugresistant(MDR) tumor cell lines
PublicationNovel 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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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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Nanoconjugates of graphene oxide derivatives and meso-tetraphenylporphyrin: a new avenue for anticancer photodynamic therapies – Cell-on-a-Chip analysis
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O-substituted tetrahydroxamate derivatives of p-tert-butylcalix[4]arene as receptors for transition and heavy metal cations
PublicationTetrasubstituted 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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Photophysical properties of 3-[2-(N-phenylcarbazolyl)benzoxazol-5-yl]alanine derivatives – experimental and theoretical studies
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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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Metabolism of antitumor 9-amino-1-nitroacridine derivatives in HepG2 cells and its influence on cytochrome P450 isoenzymes
PublicationCelem 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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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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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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Meldrum’s acid assisted formation of tetrahydroquinolin‑2‑one derivatives a short synthetic pathway to the biologically useful scaffold
PublicationA 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...