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Search results for: CARBAZOLE DERIVATIVE
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Modulation of G2 arrest enhances cell death induced by the antitumor 1-nit-roacridine derivative, Nitracrine
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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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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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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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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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Multimode systems of nonlinear equations: derivation, integrability, and numerical solutions
PublicationWe consider the propagation of electromagnetic pulses in isotropic media taking a third-order nonlinearityinto account. We develop a method for transforming Maxwell's equations based on a complete set ofprojection operators corresponding to wave-dispersion branches (in a waveguide or in matter) with thepropagation direction taken into account. The most important result of applying the method is a systemof equations describing the...
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Synthesis and antimicrobial activity of 6-sulfo-6-deoxy-D-glucosamine and its derivatives
Publication6-Sulfo-6-deoxy-D-glucosamine (GlcN6S), 6-sulfo-6-deoxy-D-glucosaminitol (ADGS) and their N-acetyl and methyl ester derivatives have been synthesized and tested as inhibitors of enzymes catalyzing reactions of the UDP-GlcNAc pathway in bacteria and yeasts. GlcN6S and ADGS at micromolar concentrations inhibited glucosamine-6-phosphate (GlcN6P) synthase of microbial origin. The former was also inhibitory towards fungal GlcN6P N-acetyl...
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Monosubstituted hydrazone β-cyclodextrin derivatives for pH-sensitive complex formation with aromatic drugs
PublicationA new and convenient synthetic pathway was developed to produce monosubstituted cyclodextrins with high yields. Each of the β-cyclodextrin derivatives described in this work has an aromatic substituent connected with cyclodextrin core by a pH-sensitive hydrazone linker and a carbon chain. Carbon chains differ in lengths having one or three carbon atoms. The correlation between water solubility and linker length was determined using...
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Photoresponsive Amide-Based Derivatives of Azobenzene-4,4′-Dicarboxylic Acid—Experimental and Theoretical Studies
PublicationAzobenzene derivatives are one of the most important molecular switches for biological and material science applications. Although these systems represent a well-known group of compounds, there remains a need to identify the factors influencing their photochemical properties in order to design azobenzene-based technologies in a rational way. In this contribution, we describe the synthesis and characterization of two novel amides...
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Xanthone synthetic derivatives with high anticandidal activity and positive mycostatic selectivity index values
PublicationWith the current massive increases in drug-resistant microbial infection as well as the significant role of fungal infections in the death toll of COVID-19, discovering new antifungals is extremely important. Natural and synthetic xanthones are promising derivatives, although only few reports have demonstrated their antifungal mechanism of action in detail. Newly synthetized by us xanthone derivative 44 exhibited strong antifungal...
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Tetrahydroquinolinone derivatives exert antiproliferative effect on lung cancer cells through apoptosis induction
PublicationThe anticancer properties of quinolones is a topic of interest among researchers in the scientific world. Because these compounds do not cause side effects, unlike the commonly used cytostatics, they are considered a promising source of new anticancer drugs. In this work, we designed a brief synthetic pathway and obtained a series of novel 8-phenyltetrahydroquinolinone derivatives functionalized with benzyl-type moieties at position...
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Skin cancer, including related pathways and therapy and the role of luteolin derivatives as potential therapeutics
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Pharmacological Profile and Molecular Modeling of Cyclic Opioid Analogues Incorporating Various Phenylalanine Derivatives
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Structure–bioavailability relationship study of genistein derivatives with antiproliferative activity on human cancer cell
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Synthesis of New Hydrazone Derivatives and Evaluation of their Efficacy as Proliferation Inhibitors in Human Cancer Cells
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Anticancer properties of ester derivatives of betulin in human metastatic melanoma cells (Me-45)
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Two novel nucleoside ester derivatives of chlorambucil as potential antileukemic prodrugs: a preliminary study
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Synthesis and photo-conversion of androsta- and pregna-5,7-dienes to vitamin D3-like derivatives
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Solvent effects on fluorescence properties of protochlorophyll and its derivatives with various porphyrin side chains
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The products of electro- and photochemical oxidation of 2-hydroxyacridinone, the reference compound of antitumor imidazoacridinone derivatives
PublicationBadano reakcje elektrochemicznego utleniania 2-hydroksyakrydonu, związku modelowego aktywnych przeciwnowotworowo pochodnych imidazoakrydonu. Do badań zastosowano metody woltamperometrii cyklicznej, metodę spektroelektrochemiczną oraz elektrolizę przy kontrolowanym potencjale. Badano też reakcje fotochemicznego utleniania. Badania prowadzono w ramach szerszego problemu poznania przemian aktywacji metabolicznej pochodnych hydroksyakrydonu...
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Indole-Acrylonitrile Derivatives as Potential Antitumor and Antimicrobial Agents—Synthesis, In Vitro and In Silico Studies
PublicationA series of 2-(1H-indol-2-yl)-3-acrylonitrile derivatives, 2a–x, 3, 4a–b, 5a–d, 6a–b, and 7, were synthesized as potential antitumor and antimicrobial agents. The structures of the prepared compounds were evaluated based on elemental analysis, IR, 1H- and 13NMR, as well as MS spectra. X-ray crystal analysis of the representative 2-(1H-indol-2-yl)-3-acrylonitrile 2l showed that the acrylonitrile double bond was Z-configured. All...
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Chemometric analysis of UV-Vis spektra of associated forms of Amphotericin B and its derivatives
PublicationPrzedmiotem badań był proces agregacji nowych pochodnych antybiotyku polienowego Amfoterycyny B. Do śledzenia procesu agregacji wykorzystano spektroskopię absorpcyjną w zakresie widzialnym i bliskiego nadfioletu. Zastosowanie zaawansowanych technik chemometrycznych pozwoliło na dogłębną analizę agregacji tych pochodnych, co pozwoliło na wyciągniecie następujacych wniosków: i) w przypadku wszystkich pochodnych przy stężeniach poniżej...
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Chromane helicity rule – scope and challenges based on an ECD study of various trolox derivatives
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The influence of different expression of CYP3A4 izoenzymes on metabolic pathway derivatives in human hepatoma cells
PublicationCelem przeprowadzonych badań było określenie różnic w metabolizmie pochodnych C-857 i C-1748 w komórkach ludzkiego nowotworu wątroby HepG2 oraz określenie wpływu na ich biotransformację w podwyższonej ekspresji izoenzymu CYP3A4 w tejże linii. Uzyskane wyniki wskazały, że związek C-857, jak również C-1748 metabolizuje w komórkach HepG2 oraz Hep3A4 do wielu reaktywnych, niestabilnych metabolitów. Różnice w biotransformacji były bardzo...
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Synthesis, spectroscopy and crystal structure determination of heteroleptic cobalt(II) silanethiolates with pyridine derivatives
PublicationCztery nowe tri-tert-butoksysilanotiolanowe kompleksy kobaltu(II) z 3- i 4-metylopirydyną zostały zsyntetyzowane i scharakteryzowane. Monometaliczne kompleksy otrzymano w reakcji bimetalicznego kompleksu [Co(SSi(OtBu)3(NH3)]2, który posłużył jako substrat kobaltu(II). Nowe związki zostały scharakteryzowane przy użyciu rentgenografii strukturalnej oraz spektroskopii UV-vis i FT-IR, a także za pomocą analizy elementarnej. Kompleksy...
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Influence of a lipid bilayer on the conformational behavior of amphotericin B derivatives - A molecular dynamics study.
PublicationAmphotericin B (AmB) is an effective but very toxic antifungal antibiotic. In our laboratory a series of AmB derivatives of improved selectivity of action was synthesized and tested. To understand molecular basis of this improvement, comparative conformational studies of amphotericin B and its two more selectivederivatives were carried out in an aqueous solution and in a lipid membrane. These molecular simulation studies revealed...
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Relationship between electronic structure and geometry of silanethiols and their derivatives. Elucidation of copper group silanethiolates
PublicationWyznaczono strukturę elektronową wybranych silanotioli X3SiSH (dla X=H, C2H5, OCH3, F, Cl i Br) oraz powstalych z nich anionów. Geometrię i funkcje falowe wyznaczono przy użyciu teorii funcjonałów gęstości elektronowej DFT. Przeanalizowano wpływ efektów anomerycznych oraz wielkości calki nakładania sigma(Si-S) na obserwowane skrócenie wiązania Si-S przy deprotonowaniu silanotioli. Podano nowe wyjaśnienie wyjątkowo niskiej kwasowości...
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Synthesis of new conjugates of MDP and nor-MDP with retro-tuftsin derivatives as potential immunomodulators
PublicationZsyntetyzowano nowe analogi muramylodipeptydu (MDP) i nor-muramylo-dipeptydu (nor-MDP) z pochodnymi retro-tuftsyny jako potencjalne immunomodulatory. Przedstawiono także syntezę odpowiednich pochodnych retro-tuftsyny. Do syntezy wykorzystano metodę mieszanych bezwodników z chloromrówczanem izobutylu i N-metylomorfoliną w bezwodnym DMF.
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Chapter 22. Antimicrobial and surface activity of 1-alkyl-3-methyl imidazolium derivatives
PublicationCiecze jonowe wykazują aktywność przeciwgrzybową oraz przeciwbakteryjną zależną od struktury badanego związku. Zbadano wpływ długości łańcucha alkilowego w kationie na aktywność przeciwmikrobiologiczną oraz przedstawiono zależność pomiędzy tą aktywnością a krytycznym stężeniem micelizacji imidazolowych cieczy jonowych.
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An In Vitro Antimicrobial, Anticancer and Antioxidant Activity of N–[(2–Arylmethylthio)phenylsulfonyl]cinnamamide Derivatives
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Can Immobilized Artificial Membrane Chromatography Support the Characterization of Antimicrobial Peptide Origin Derivatives?
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Effect of thienyl units in cyanoacrylic acid derivatives toward dye-sensitized solar cells
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Preliminary antifungal activity assay of selected chlorine-containing derivatives of xanthone and phenoxyethyl amines
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Conformational Preferences of Proline Derivatives Incorporated into Vasopressin Analogues: NMR and Molecular Modelling Studies
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Sensorless IPMSM drive with rotor position estimator based on analysis of phase current derivatives
PublicationThis paper describes a sensorless Interior Permanent Magnet Synchronous Motor (IPMSM) drive designed for traction applications. Wide-speed sensorless operation is provided with the use of three methods of rotor position estimation designed for: a standstill, low- and high-speed range. The paper focuses on the high-speed estimation algorithm. The estimator uses the derivatives of motor phase currentsresulting from PWM modulation...
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Synthesis of phosphono and phosphate derivatives of hydroxyimino-D-alditols as new potential antifungal agents
PublicationIn search for new effective we antyfungals we focus on two enzymes involved in biosynthesis of the fungal cell wall. The first enzyme is glucosamine-6-phosphate (GlmS), which catalyzes transformation of D-fructose-6-phosphate (Fru-6P) to D-glucosamine-6-phodphate (GlcN-6P) in the chitin biosynthesis pathway. The second enzyme is phosphomannose isomerase (PMI) repored to play a crucial role in biosynthesis of many mannosylated structures,...
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Synthesis of disubstituted 1,3,4,9-tetrahydropyrano-[3,4-b]indole-1-acetic acids derivatives
Publication1,3,4,9-tetrahydropyrano[3,4-b ]indole-1-acetic acid derivatives are of interest for pharmaceutical research as a core structure for synthesis of biological active substance - Etodolac (selective Cyclooxygenase-2 inhibitor, which belongs to the Non-steroidal Anti-inflammatory Drug, NSAID, that shows a clin-ically effective analgesic and anti-inflammatory activity). Here the way of synthesis of two 1,3,4,9-tetrahydropyrano[3,4-b...
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Thermal Decomposition of Carbamoyl Meldrum’s Acids: A Starting Point for the Preparation of 1,3-Oxazine Derivatives
PublicationThe ability to undergo [4 + 2] versus [2 + 2] cycloaddition was under investigation for ketenes thermally generated from carbamoyl Meldrum’s acid. Usually, 1,3-oxazino-5-carbamoylo-4,6-diones are formed when carbamoyl Meldrum’s acid reacts with imine. However, in some cases, a reaction takes an unexpected course, leading to the formation of tetraponerines alkaloids derivatives or cyclic iminoethers.
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Synthesis of functionalized new conjugates of batracylin with tuftsin/ retro-tuftsin derivatives and their biological evaluation
PublicationNew batracylin conjugates with tuftsin/retro-tuftsin derivatives were designed and synthesized using T3P as a coupling agent. The conjugates possess an amide bond formed between the carboxyl group of heterocyclic molecule and the N-termini of the tuftsin/retro-tuftsin chain. The in vitro cytotoxic activity of the new analogues and their precursors was evaluated using a series of human and murine tumor cells. BAT conjugates containing...
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Synthesis and antiproliferative activity of conjugates of adenosine with muramyl dipeptide and nor-muramyl dipeptide derivatives
PublicationWe synthesized a series of MDP(D,D) and nor-MDP(D,D) derivatives conjugated with adenosine through a spacer as potential immunosuppressants. New conjugates were evaluated on two leukemia cell lines (Jurkat and L1210) and PBMC from healthy donors.
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Synthesis of conjugates of muramyl dipeptide and nor-muramyl dipeptide derivatives with adenosine as potential immunosuppressant
PublicationZaprezentowano syntezę koniugatów adenozyny z pochodnymi muramylo- i nor-muramylodipeptydów zawierających w części peptydowej D-aminokwasy (D-Ala, D-Val, D-Ser, D-Pro, D-2-ABA). Jako substrat zastosowano rybozyd 6-chloropuryny, który łączono poprzez 1,2-diaminoetan z odpowiednimi pochodnymi MDP lub nor-MDP w obecności EDCI i HOBt. Struktury otrzymanych związków zostały potwierdzone widmami 1H i 13C NMR (500 MHz), widmami MS oraz...
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Synthesis of conjugates of muramyl dipeptide and nor-muramyl dipeptide derivatives with adenosine as potential immunosuppressants
PublicationPrzedstawiono syntezę koniugatów pochodnych muramylodipeptydu (MDP) i nor-MDP z adenozyną jako potencjalnych związków o działaniu immunosupresyjnym. Jako substrat zastosowano rybozyd 6-chloropuryny, który łączonp poprzez 1,2-diaminoetan z pochodną MDP lub nor-MDP. Do syntezy wykorzystano pochodne MDP zawierające w części peptydowej D-aminokwasy (D-Ala, D-Val, D-Ser, D-Pro, D-2-ABA). Jako odczynniki sprzęgające zastosowano EDCI...
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Improving the regulation of the derivatives market as an objective prerequisite for sustainable development of the global financial system
PublicationThe development of financial markets is characterized by the emergence of new financial instruments, in particular derivatives, the risk level analysis of which is complicated. Counterparties are not always fully aware of and do not adequately assess the potential risks of derivatives, which may lead to large financial losses and sometimes bankruptcies. The purpose of the study is to generalize approaches to regulating derivative...
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Effect of chemical structure on complexation efficiency of aromatic drugs with cyclodextrins: The example of dibenzazepine derivatives
PublicationIt is widely believed that the hydrophobic effect governs the binding of guest molecules to cyclodextrins (CDs). However, it is also known that high hydrophobicity of guest molecules does not always translate to the formation of stable inclusion complexes with CDs. Indeed, a plethora of other factors can play a role in the efficiency of guest–CD interactions, rendering structure-based prediction of the complexation efficiency with...
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Novel N-(aryl/heteroaryl)-2-chlorobenzenesulfonamide derivatives: synthesis and anticancer activity evaluation
PublicationA new series of N-(aryl/heteroaryl)-2-chlorobenzenesulfonamide derivatives 4-21 have been synthesized, and evaluated at the National Cancer Institute (USA) for their in vitro activities against a panel of 60 different human cancer cell lines. Among them, compounds 16, 20 and 21 exhibited remarkable cytotoxic activity against numerous human cancer cell lines. We found that sulfonamide derivative 21 appeared to be more selective...
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A new 1-nitro-9-aminoacridine derivative targeting yeast topoisomerase II able to overcome fluconazole-resistance
PublicationFungal resistance remains a significant threat and a leading cause of death worldwide. Thus, overcoming microbial infections have again become a serious clinical problem. Although acridine derivatives are widely analyzed as anticancer agents, only a few reports have demonstrated their antifungal activity. In an effort to develop biologically active antifungals, twelve novel C-857 (9-(2′ -hydroxyethylamino)-1-nitroacridine) and...
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Construction of heterometallic and mixed-valence copper(I/II) chloride π-complexes with 1,2,4-triazole allyl-derivative
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Sensitive Demonstration of the Twin-Core Couplers including Kerr Law Non-Linearity via Beta Derivative Evolution
PublicationTo obtain new solitary wave solutions for non-linear directional couplers using optical meta-materials, a new extended direct algebraic technique (EDAT) is used. This model investigates solitary wave propagation inside a fiber. As a result, twin couplers are the subject of this study. Kerr law is the sort of non-linearity addressed there. Because it offers solutions to problems with large tails or infinite fluctuations, the resulting...