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Search results for: BISACRIDINE DERIVATIVES
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Determining the true content of quercetin and its derivatives in plants employing SSDM and LC–MS analysis
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Diosgenyl 2-amino-2-deoxy-β-D-galactopyranoside: synthesis, derivatives and antimicrobial activity
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Fragmental Method KowWIN as the Powerful Tool for Prediction of Chromatographic Behavior of Novel Bioactive Urea Derivatives
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The oxydiacetate and iminodiacetate complexes of oxidovanadium(IV) as the new series of the catalysts for the oligomerization of beta-olefin derivatives
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Molecular modeling and evaluation of novel dibenzopyrrole derivatives as telomerase inhibitors and potential drug for cancer therapy
PublicationDuring previous years, many studies on synthesis, as well as on anti-tumor, anti-inflammatory and anti-bacterial activities of the pyrazole derivatives have been described. Certain pyrazole derivatives exhibit important pharmacological activities and have proved to be useful template in drug research. Considering importance of pyrazole template, in current work the series of novel inhibitors were designed by replacing central...
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Opioid Growth Factor and its Derivatives as Potential Non-toxic Multifunctional Anticancer and Analgesic Compounds
PublicationIn this paper, we review the structure-activity relationship of OGF and its analogues. We highlight also OGF derivatives with analgesic, immunomodulatory activity and the ability to penetrate the blood-brain barrier and may be used as safe agents enhancing chemotherapy efficacy and improving quality of life in cancer patients. The reviewed papers indicate that Met-enkephalin and its analogues are interesting candidates for the...
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Elucidating the impact of enzymatic modifications on the structure, properties, and applications of cellulose, chitosan, starch and their derivatives: a review
PublicationPolysaccharides, as one of the most prominent natural biopolymers, display numerous biological activities and industrial applications. Nevertheless, some polysaccharides lack biological properties or display weak biological activities. Besides, practical usages of polysaccharides still remain challenging because of their poor solubility and inappropriate hydrophilic/hydrophobic balance. Hence, enzymatic or chemical modifications...
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Comments on various extensions of the Riemann–Liouville fractional derivatives : About the Leibniz and chain rule properties
PublicationStarting from the Riemann–Liouville derivative, many authors have built their own notion of fractional derivative in order to avoid some classical difficulties like a non zero derivative for a constant function or a rather complicated analogue of the Leibniz relation. Discussing in full generality the existence of such operator over continuous functions, we derive some obstruction Lemma which can be used to prove the triviality...
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General, Mild, and Metal-Free Functionalization of Indole and Its Derivatives Through Direct C3-Selenylation
PublicationA very mild method for the introduction of functionalized alkylselenyl group at C-3 position of the indole ring was developed. The proposed procedure consists of an electrophilic substitution of indole and its derivatives with bis(O,O-diisopropoxyphosphorothioyl) diselenide and subsequent cleavage of the P–Se bond with tetrabutylammonium fluoride in the presence of various electrophilic reagents. This method can be successfully...
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Investigation of the Binding Properties of the Cosmetic Peptide Argireline and Its Derivatives Towards Copper(II) Ions
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Antitumor Activity of Novel Benzensulfonamide Derivatives in View of their Physiochemical Properties Searched by Principal Component Analysis
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Derivatives of 1-nitroacridine induce apoptosis only in a limited number of human colon adenocarcinoma cells
PublicationPraca dotyczy indukcji apoptozy w komórkach ludzkich raków okrężnicy HT29 i HCT8 pod wpływem pochodnych 1-nitroakrydyny: C-857 i C-1748. Wykazano, że związki te w stężeniach biologicznie istotnych (EC90) indukują apoptozę tylko w części populacji komórek. Efekt ten uzależniony był od czasu inkubacji komórek ze związkiem, a nie zależał od stężenia związku.
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Inactivation of glucosamine-6-phosphate synthase by N3-oxoacyl derivatives of L-2,3-diaminopropanoic acid
PublicationN3-oksoacylowe pochodne kwasu l-2,3-diaminopropanowego zawierające ugrupowanie epoksydowe lub układ sprzężonych wiązań podwójnych inaktywują syntaze glukozamino-6-fosforanu (GlcN-6-P) z S. cerevisiae. Wyniki badań kinetycznych inaktywacji enzymu wskazują na dwuetapowy przebieg tej reakcji, przy czym tworzenie kompleksu enzym:ligand poprzedza nieodwracalną modyfikację enzymu. Badane związki różniły się powinowactwem do centrum aktywnego...
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Chromogenic derivatives of new bis(phenylhydrazono-1H-tetrazol-5-yl-acetonitriles) - synthesis and properties
PublicationDerivatives of bis(phenylhydrazono-1H-tetrazol-5-yl-acetonitriles) with oxygen and sulphur atoms in the structure of aliphatic chains were successfully synthesised. The correlation between the ligand structure and its complexation properties was investigated by absorption spectroscopy. The formation of complexes of presented compounds with metal cations (Cu2+, Ni2+, Zn2+, Co2+, Fe2+ and Pb2+) was studied. Ligands 5-8 were additionally...
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Synthesis and biological activity of novel mycophenolic acid conjugates containing nitro-acridine/acridone derivatives
PublicationOpracowano warunki reakcji kwasu mykofenolowego z aminowymi pochodnymi akrydyn i akrydonów. Tak otrzymane koniugaty zostały scharakteryzowane, a następnie przebadane in vitro pod względem aktywności przeciwbiałaczkowej oraz immunosupresyjnej.
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Synthesis and biological activity of ester derivatives of mycophenolic acid and acridines/acridones as potential immunosuppressive agents
PublicationImproved derivatives of mycophenolic acid (MPA) are necessary to reduce the frequency of adverse effects, this drug exerts in treated patients. In this study, MPA was coupled with N-(x-hydroxyalkyl)-9-acridone-4-carboxamides or N-(x-hydroxyalkyl)acridine-4-carboxamides to give respective ester conjugates upon Yamaguchi protocol. This esterification required protection of phenol group in MPA. Designed conjugates revealed higher...
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NADES propolis extracts - update 2023 and synthesis of derivatives of propolis ingredients
Open Research DataThis dataset contains results of our investigation aiming in determination of antimicrobial potential of the propolis extracts produced with deep eutectic solvents
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Fractional Variable-Order Derivative and Difference Operators and Their Applications to Dynamical Systems Modelling
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Multiple Solutions to Third-Order Differential Equations with Derivative Dependence and Deviating Arguments
PublicationIn this paper, we give some new results for multiplicity of positive (nonnegative) solutions for third-order differential equations with derivative dependence, deviating arguments and Stieltjes integral boundary conditions. We discuss our problem with advanced argument α and arbitrary β ∈ C([0,1],[0,1]), see problem (2). It means that argument β can change the character on [0,1], so β can be delayed in some set J ⊂ [0,1] and advanced...
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Enantioselective sensing of (S)-Thalidomide in blood plasma with a chiral naphthalene diimide derivative
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Apoptosis of human leukemia cells induced by imidazoacridinone derivative C-1311 (Symadex)
PublicationPraca dotyczy różnej wrażliwości komórek białaczek ludzkich do ulegania apoptozie pod wpływem pochodnej imidazoakrydonu C-1311, co jest zgodne z aktywnością cytotoksyczną tego związku (EC90) wobec badanych komórek.
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The Effect of Conjugation with Octaarginine, a Cell-Penetrating Peptide on Antifungal Activity of Imidazoacridinone Derivative
PublicationAcridine cell-penetrating peptide conjugates are an extremely important family of compounds in antitumor chemotherapy. These conjugates are not so widely analysed in antimicrobial therapy, although bioactive peptides could be used as nanocarriers to smuggle antimicrobial compounds. An octaarginine conjugate of an imidazoacridinone derivative (Compound 1-R8) synthetized by us exhibited high antifungal activity against reference...
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Carbon Nanotubes Derivatized with Mediators for Laccase Catalyzed Oxygen Reduction.
PublicationPrzedstawiono konstrukcję elektrody w której wykorzystano nanorurki modyfikowane znanym mediatorem (ABTS). Cząsteczki mediatora przyłączono do ścian bocznych nanorurek oraz do ich końców. Porównano parametry elektrod zbudowanych w oparciu o nanorurki modyfikowane kowalencyjnie w różny sposób. Zaobserwowano pozytywny wpływ modyfikowanych nanorurek na parametry elektrody.
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Inner derivations of special subrings of matrix rings and outerplanar digraphs.
PublicationTematem artykułu jest specjalny podpierścień pierścienia macierzy wyznaczony przez relację oraz digraf reprezentujący tę relację. Rozważane są takie relacje, dla których reprezentujące je digrafy są zewnętrznie planarne. W tym przypadku zostały udowodnione warunki konieczne i wystarczające na to, aby różniczkowanie pierścienia było wewnętrzne.
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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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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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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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Synthesis and Thermal, Photophysical, Electrochemical Properties of 3,3-di[3-Arylcarbazol-9-ylmethyl]oxetane Derivatives
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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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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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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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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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Exploring Alkyl Ester Salts of L-Amino Acid Derivatives of Ibuprofen: Physicochemical Characterization and Transdermal Potential
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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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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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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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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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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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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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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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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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CYP3A4 overexpression enhances the cytotoxicity of the antitumor triazoloacridinone derivative C-1305 in CHO cells
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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...