Search results for: TETRAHYDROQUINOLINONE DERIVATIVES
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Metabolism of antitumour agent 1-nitroacridine derivative, C-1748 in pancreatic cancer cell lines
PublicationPancreatic 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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Antitumor 1-nitroacridine derivative C-1748 induces significant apoptosis in pancreatic cancer cells.
PublicationPancreatic 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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Numerical and quantitative analysis of HIV/AIDS model with modified Atangana-Baleanu in Caputo sense derivative
PublicationFractional 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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Chitin and derivative chitosan-based structures — Preparation strategies aided by deep eutectic solvents: A review
PublicationThe high molecular weight of chitin, as a biopolymer, challenges its extraction due to its insolubility in the solvents. Also, chitosan, as the N-deacetylated form of chitin, can be employed as a primary material for different industries. The low mechanical stability and poor plasticity of chitosan films, as a result of incompatible interaction between chitosan and the used solvent, have limited its industrialization. Deep eutectic...
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Interactions of amphotericin B derivative of low toxicity with biological membrane components - the Langmuir monolayer approach
PublicationMetodą 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...
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Preliminary Investigation of the Antibacterial Activity of Antitumor Drug 3-Amino-1,2,4-Benzotriazine-1,4-Dioxide (Tirapazamine) and its Derivatives
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Molecular modeling of Gram-positive bacteria peptidoglycan layer, selected glycopeptide antibiotics and vancomycin derivatives modified with sugar moieties
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IR–Raman, NMR and density functional methods in the examination of tautomerism and features of N-methyl substituted 9-acridinamine derivatives
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Copper(I) π-coordination compounds with allyl derivatives of disubstituted pseudothiohydantoin: synthesis, structure investigation and nonlinear optical features
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Physicochemical profile of Os (III) complexes with pyrazine derivatives: From solution behavior to DNA binding studies and biological assay
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Synthesis and Properties of Di-isopropylamino Derivatives of Diphosphanes and Triphosphanes: The X-Ray Structure of (iPr2N)2P-P(SiMe3)2
PublicationPrzeprowadzono reakcję (iPr2N)2PCl z P(SiMe3)2Li w wyniku której otrzymano difosfan (iPr2N)2P-P(SiMe3)2. Strukturę związku określono przy pomocy rentgenowskiej analizy strukturalnej. Otrzymano także pochodną litową (iPr2N)2P-P(SiMe3)Li w rekcji z nBuLi. W reakcji (iPr2N)2PCl z (iPr2N)2P-P(SiMe3)Li otrzymano trifosfan (iPr2N)2P-P(SiMe3)-P(NiPr2)2 z dużą wydajnością. Próby otrzymania pochodnej litowej (iPr2N)2P-PLi-P(NiPr2)2 zakończyły...
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Esters of p-nitrophenol in synthesis of 1-N-monoamide and 1,7-bis-N,N-amide derivatives of 1,4,7,10-tetraazacyclododecane
PublicationW artykule opisana została synteza acylowych pochodnych 1,4,7,10-tetraazacyklododekanu przy pomocy estrów aktywnych. W bezpośredniej reakcji estrów 4-nitrofenylowych z cyklenem prowadzonej w bardzo łagodnych warunkach otrzymano pochodne mono i dipodstawienia z bardzo dobrymi wydajnościami. Zbadano również wpływ różnych parametrów na dystrybucję produktów.
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Cytochrome P450 izoenzymes involved in metabolism of antitumor 9-amino-1-nitroacridine derivatives, C-857, C-1748
PublicationPraca jest częścią szerszych badań zmierzających do poznania molekularnego mechanizmu metabolicznej transformacji przeciwnowotworowych pochodnych 9-amino-1-nitroakrydyny. W naszym zespole wyselekcjonowano pochodną nowej generacji, która w porównaniu z poprzednimi wykazała znacznie obniżoną toksyczność ogólną. W wyniku przeprowadzonych badań wykazaliśmy, że nowa pochodna jest znacznie mniej podatna na metabolizm katalizowany przez...
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Photodynamic Inactivation of Bacteria with Porphyrin Derivatives: Effect of Charge, Lipophilicity, ROS Generation, and Cellular Uptake on Their Biological Activity In Vitro
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Diamine derivatives of dimerized fatty acids and bio-based polyether polyol as sustainable platforms for the synthesis of non-isocyanate polyurethanes
PublicationA series of environmentally friendly non-isocyanate polyurethanes (NIPUs) were successfully prepared via the polyaddition reaction of bio-based polyether polyol-based cyclic carbonate with diamine derivative of dimerized fatty acids. The syntheses of NIPUs were realized by the three-step method in the absence of toxic solvents and, importantly, the process of carbonation did not require the use of elevated pressure. The effect...
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Structural, spectral and magnetic properties of Ni(II), Co(II) and Cd(II) compounds with imidazole derivatives and silanethiolate ligands
PublicationA series of new metal heteroleptic complexes have been obtained in simple reactions of 1-(3-aminopropyl)-imidazole (api) and 1,4-bis(imidazol-1-yl)-butane (bbi) ligands with metal silanethiolates or acetylacetonates. The obtained complexes are the coordination polymers [Ni{SSi(tBuO)3}2(μ-api)]n1, [Co{SSi(tBuO)3}2(μ-api)]n2, [Cd{SSi(tBuO)3}2(μ-api)·2CH3OH]n3, [Cd{SSi(tBuO)3}2(μ-bbi)·CHCl3]n4 and the dimer [Co{SSi(tBuO)3}2(μ-bbi)·3CH3OH]25....
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RP-HPLC WITH DETECTION BY MEANS OF ESI-MS AND UV FOR IDENTIFICATION OF CHROMATOGRAPHIC PEAKS OF SOME HYDROXY DERIVATIVES OF EPOXY RESIN
PublicationThe composition of products synthesized on the basis of ED-24 epoxy resin has been studied using a reversed phase high-performance liquid chromatography followed by an electrospray ionization mass spectrometry (RP-HPLC/ESI-MS). The synthesized products contain free hydroxy groups and such groups, as epoxy, peroxy, carboxy or acrylate.
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Novel Nystatin A1 derivatives exhibiting low host cell toxicity and antifungal activity in an in vitro model of oral candidosis
PublicationOpportunistic oral infections caused by Candida albicans are frequent problems in immunocompromised patients. Management of such infections is limited due to the low number of antifungal drugs available, their relatively high toxicity and the emergence of antifungal resistance. Given these issues, our investigations have focused on novel derivatives of the antifungal antibiotic Nystatin A1, generated by modifications at the amino...
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Nonnegative solutions to nonlocal boundary value problems for systems of second-order differential equations dependent on the first-order derivatives
PublicationStosując tw. Avery-Petersona o punkcie stałym, podano warunki dostateczne na istnienie nieujemnych rozwiązań dla układów równań różniczkowych rzędu drugiego z argumentami opóźnionymi i wyprzedzonymi oraz warunkami brzegowymi zawierającymi całki Stieltjesa. Praca zawiera wiele przykładów.
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Studies on Aminoanthraquinone-Modified Glassy Carbon Electrode: Synthesis and Electrochemical Performance toward Oxygen Reduction
PublicationIn this paper, 9,10-anthraquinone (AQ) derivative-modified glassy carbon (GC) electrodes were studied towards the electrochemical reduction of oxygen in aqueous and non-aqueous solutions. The reaction of 1-chloro-9,10-anthraquinone with aliphatic diamines was applied for the synthesis of amino-9,10-anthraquinone derivatives. The obtained AQ derivatives were grafted onto the surface of glassy carbon electrodes by electropolymerisation...
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Carbon nanotubes chemically derivatized with rebox systems as mediators for biofuel cell applications
PublicationEnzymatyczne bioogniwa paliwowe to urządzenia wykorzystujące enzymy do przemiany energii chemicznej w elektryczną. Zyskana w ten sposób energia może służyć do zasilania wszczepialnych urządzeń (np. czujników glukozy, rozruszników serca).Przedstawiono sposób otrzymywania i właściwości bioelektrod, w których wykorzystano nanorurki węglowe modyfikowane mediatorami enzymatycznych reakcji redoks. Do nanorurek przyłączano zarówno mediatory...
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Carbon Nanotubes Chemically Derivatized with Redox Systems as Mediators for Biofuel Cell Applications
PublicationEnzymatyczne bioogniwa paliwowe to urządzenia wykorzystujące enzymy do przemiany energii chemicznej w elektryczną. Zyskana w ten sposób energia może służyć do zasilania wszczepialnych urządzeń (np. czujników glukozy, rozruszników serca). Przedstawiono sposób otrzymywania i właściwości bioelektrod, w których wykorzystano nanorurki węglowe modyfikowane mediatorami enzymatycznych reakcji redoks. Do nanorurek przyłączano zarówno mediatory...
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On the dervative of the Legendre function of the first kind with respect to its degree [Corrigendum]
PublicationSkorygowano błąd matematyczny w pracy: R. Szmytkowski, On the derivative of the Legendre function of the first kind with respect to its degree, J. Phys. A: Math. Gen. Vol. 39(2006) s. 15147-15172 [744014]
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Studies on Aminoanthraquinone-Modified Glassy Carbon Electrode: Synthesis and Electrochemical Performance toward Oxygen Reduction
PublicationIn this paper, 9,10-anthraquinone (AQ) derivative-modified glassy carbon (GC) electrodes werestudied towards the electrochemical reduction of oxygen in aqueous and non-aqueous solutions. The reaction of 1-chloro-9,10-anthraquinone with aliphatic diamines was applied for the synthesis of amino-9,10-anthraquinone derivatives. The obtained AQ derivatives were grafted onto the surface of glassy carbon electrodes by electropolymerisation...
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Mirosław Andrusiewicz prof. dr hab. n. med. i n. o zdr.
PeopleDiplomas, degrees conferred in specific areas ̶ Post-doctoral degree in medical sciences (doctor habilitated) (discipline: medical biology) December 4, 2017; Title of academic achievement: "Analysis of selected genes involved in the control of pathological changes in cells derived from internal female reproductive organs"; Poznan University of Medical Sciences, Faculty of Medicine II; re-viewers: Prof. Katarzyna Ziemnicka,...
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Ultrasound assisted rapid synthesis of mefenamic acid based indole derivatives under ligand free Cu-catalysis: Their pharmacological evaluation
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Selective transport of zinc ions through novel polymer inclusion membranes (PIMS) containing β-diketone derivatives as carrier reagents
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Kinetics of adsorption of hydrocarbon chloro-derivatives from seven-component aqueous solution onto a thin layer of DTO-activated carbon
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Pharmacological Classification and Activity Evaluation of Furan and Thiophene Amide Derivatives Applying Semi-Empirical ab initio Molecular Modeling Methods
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Lipophilicity Determination of Antifungal Isoxazolo[3,4-b]pyridin-3(1H)-ones and Their N1-Substituted Derivatives with Chromatographic and Computational Methods
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Imidazolidine-4-one derivatives in the search for novel chemosensitizers of Staphylococcus aureus MRSA: Synthesis, biological evaluation and molecular modeling studies
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Discovery of Novel 3-Hydroxyandrosta-5,7-Diene-17-Carboxylic Acid Derivatives as Anti-Inflammatory Bowel Diseases (IBD) Agents
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Amberlyst-15 catalysed synthesis of novel indole derivatives under ultrasound irradiation: Their evaluation as serotonin 5‑HT2C receptor agonists
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New conjugates of muramyl dipeptide and nor-muramyl dipeptide linked to tuftsin and retro-tuftsin derivatives significantly influence their biological activity
PublicationOpisano syntezę nowych koniugatów MDP i nor-MDP z pochodnymi tuftsyny i retro-tuftsyny zawierającymi wiązanie izopeptydowe pomiędzy epsilon-aminową grupą lizyny, a karboksylową grupą Ala, Gly czy Val. Zbadano ich aktywność biologiczną, m.in. profil cytokinowy.
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Novel 1,2,3-Triazole Derivatives as Mimics of Steroidal System—Synthesis, Crystal Structures Determination, Hirshfeld Surfaces Analysis and Molecular Docking
PublicationHerein, we present the synthesis and crystal structures determination of five 4-(1-phenyl-1H-1,2,3-triazol-4-yl)phenol derivatives containing halogen atoms, 6a–e, which may be used as an excellent mimic of steroids in the drug development process. Good quality crystals obtained for all of the synthesized compounds allowed the analysis of their molecular structures. Subsequently, the determined crystal structures were used to calculate...
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Amberlyst-15 catalysed synthesis of novel indole derivatives under ultrasound irradiation: Their evaluation as serotonin 5‑HT2C receptor agonists
PublicationA series of indole based novel Schiff bases was designed as potential agonists of 5‑HT2C receptor that was supported by docking studies in silico. These compounds were synthesized via Amberlyst-15 catalysed condensation of an appropriate pyrazole based primary amine with the corresponding indole-3-aldehyde under ultrasound irradiation at ambient temperature. A number of target Schiff bases were obtained...
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Design, synthesis and biological evaluation of novel N-phosphorylated and O-phosphorylated tacrine derivatives as potential drugs against Alzheimer’s disease
PublicationIn this work, we designed, synthesised and biologically investigated a novel series of 14N- and O-phosphorylated tacrine derivatives as potential anti-Alzheimer’s disease agents. In the reaction of 9-chlorotacrine and corresponding diamines/aminoalkylalcohol we obtained diamino and aminoalkylhydroxy tacrine derivatives. Next, the compounds were acid to give final products 6–13 and 16–21 that were characterised by 1H, 13 C, 31P...
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The comparison of antioxidant properties and nutrigenomic redox-related activities of vitamin C, C-vitamers, and other common ascorbic acid derivatives
PublicationThe term ‘vitamin C’ describes a group of compounds with antiscorbutic activity of L-ascorbic acid (AA). Despite AA’s omnipresence in plant-derived foods, its derivatives have also been successfully implemented in the food industry as antioxidants, including the D-isomers, which lack vitamin C activity. This study aimed to determine the relationship between redox-related activities for five derivatives of AA using electrochemical,...
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Computational analysis of substituent effects on proton affinity and gas-phase basicity of TEMPO derivatives and their hydrogen bonding interactions with water molecules
PublicationThe study investigates the molecular structure of 2,2,6,6-tetramethylpiperidine-1-oxyl (TEMPO) and its derivatives in the gas phase using B3LYP and M06-2X functional methods. Intermolecular interactions are analyzed using natural bond orbital (NBO) and atoms in molecules (AIM) techniques. NO2-substituted TEMPO displays high reactivity, less stability, and softer properties. The study reveals that the stability of TEMPO derivatives...
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Novel fused pyran derivatives induce apoptosis and target cell cycle progression in anticancer efficacy against multiple cell lines.
PublicationNitrogen-based heterocycles such as pyrazole, imidazole, 1,2,4-triazole, benzimidazole, and benzotriazole substituted fused pyran derivatives (6a–e, 8a–e, 10a–e, 12a–e,&14a–e) have been synthesized and tested for their in vitro anticancer efficacies against MCF7, A549, and HCT116 cancer cell lines. Among the compounds, 6e, 14b, and 8c were identified as the most potent against MCF7, A549, and HCT116, with IC50 values of 12.46 2.72...
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Amphotericin B derivatives: novel strategy for the development of non-toxic, broad spectrum, fungicidal and overcoming multidrug resistance antifungal agents.
PublicationZaprezentowano porównawczą charakterystykę działania amfoterycyny B (AmB) oraz jej pochodnych o różnym stopniu selektywnej toksyczności na szczepy grzybów reperezentujących różne mechanizmy oporności. Były to mutanty C. albicans posiadające defekt w szlaku biosyntezy ergosterolu oraz wielolekooporne szczepy S. cerevisiae wyposażone w pompy eksportujące typu ABC i MFS. Badania obejmowały: 1)porównanie aktywności przeciwgrzybowej...
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The influence of 4-substituted and unsubstituted derivatives of 1-nitroacridine on the cell cycle and induction of apoptosis in human cancer HT29 and HeLa S3.
PublicationZbadano wpływ pochodnych 1-nitroakrydyny C-1748 i C-857, w stężeniach biologicznie istotnych, na cykl życiowy oraz indukcję apoptozy komórek raka jelita grubego HT29 oraz raka szyjki macicy HeLa S3. Metodą cytometrii przepływowej wykazano, że 4-metylo-1-nitroakrydyna C-1748 powoduje akumulację komórek HT29 w fazie S i komórek HeLa S3 w fazie G2 cyklu komórkowego zaś związek C-857 indukuje akumulację komórek HT29 i HeLa S3 w fazie...
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The response of human colon cancer cells to C-1748 (4-methyl-1-nitroacridine derivative) treatment
PublicationPrzeprowadzone badania miały na celu określenie wpływu pochodnej 4-metylo-1-nitroakrydyny C-1748 na komórki ludzkiego raka okrężnicy HCT8 oraz HT29. Komórki obu linii, traktowane badanym związkiem, ulegały przede wszystkim apoptozie, przy czym liczba komórek apoptotycznych była znacznie większa w przypadku linii HCT8. Ponadto, proliferacja części komórek HCT8, została zahamowana w wyniku uruchomienia procesu starzenia, czego nie...
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Preclinical toxicological examination of a putative prostate cancer-specific 4-methyl-1-nitroacridine derivative in rodents
PublicationW pracy przedstawiono wyniki przedklinicznych badań toksykologicznych zwiazków C-1748 i C-857 na szczurach Copenhagen i myszach BALB/c, po podaniu dootrzewnowym lub dożylnym. U myszy dawki letalne (LD50) dla C-1748 wynosiły odpowiednio 9 i 13,4 mg/kg w porównaniu z 2,2 i 3 mg/kg dla C-857. U szczurów po podaniu dootrzewnowym lub dożylnym dla C-1748 dawki LD50 wynosiły odpowiednio 4 i 1,3 mg/kg. Nie stwierdzono zmian w liczbie komórek...
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Advancement of Non-Newtonian Fluid with Hybrid Nanoparticles in a Convective Channel and Prabhakar’s Fractional Derivative—Analytical Solution
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Proportional-Derivative and Model-based Controllers used for a Serial Type Manipulator in case of a Variable Mass Payload
PublicationIn the paper, numerical analysis of dynamics of a variable mass system is considered. Its reference example is a serial-like manipulator composed of revolute joints and rigid bodies. Payload of its gripper is considered as its variable mass element (mass and inertia irregularly between subsequent payloads). For the rest of the system, inertia parameters are considered as known (precisely identified during the assembling process)....
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Collaboration between a proportional-derivative and a model-based controllers in case of a variable mass redundantly articulated manipulators
PublicationW pracy zaprezentowano wyniki analizy numerycznej dynamiki złożonego układu mechatroniczego. Częścią mechaniczną analizowanego układu jest manipulator sterowany nadmiarowo. Rozważania ograniczono do analizy płaskiego manipulatora równoległego. Część sterująca to układ sterowania (regulacji) z modelem. Analizowane zadanie polega na wymuszeniu ruchu wzdłuż zadanej trajektorii. Problemy związane ze sterowaniem prowadzą nas do pierwszego...
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Positive solutions to second-order differential equations with dependence on the first-order derivative and nonlocal boundary conditions
PublicationIn this paper, we consider the existence of positive solutions for second-order differential equations with deviating arguments and nonlocal boundary conditions. By the fixed point theorem due to Avery and Peterson, we provide sufficient conditions under which such boundary value problems have at least three positive solutions. We discuss our problem both for delayed and advanced arguments α and also in the case when α(t)=t, t∈[0,1]....
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Modulation of G2 arrest enhances cell death induced by the antitumor 1-nit-roacridine derivative, Nitracrine
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Carbon Nanotubes Chemically Derivatize with Redox Systems as Mediators for Biofel Cell Applicatoions
PublicationEnzymatyczne bioogniwa paliwowe to urządzenia wykorzystujące enzymy do przemiany energii chemicznej w elektryczną. Zyskana w ten sposób energia może służyć do zasilania wszczepialnych urządzeń (np. czujników glukozy, rozruszników serca).Przedstawiono sposób otrzymywania i właściwości bioelektrod, w których wykorzystano nanorurki węglowe modyfikowane mediatorami enzymatycznych reakcji redoks. Do nanorurek przyłączano zarówno mediatory...