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Search results for: ANTITUMOUR AGENT
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SYNTHESIS OF PHOSPHORUS TACRINE ANALOGUES AS A NEW POTENTIAL ANTI-ALZHEIMER’S DISEASE AGENTS
PublicationA series of novel phosphorus tacrine derivatives was obtained in three steps, including synthesis of 9-chlorotacrine, connection of 9-chlorotacrine with hexamethylenediamine, 1,8-diaminooctane and 1,12-diaminododecane linkers and reaction of obtained tacrine diamine analogues with corresponding acid ester to give nine tacrine organophosphorus compounds. All of the obtained final structures were characterized by 1H NMR, 13C NMR,...
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Ruthenium(II) and Iridium(III) Complexes as Tested Materials for New Anticancer Agents
PublicationThe oncological use of cisplatin is hindered by its severe side eects and a very important resistance problem. To overcome these problems, scientists have attempted to design new generation transition-metal anticancer complexes. In this study, we present new complexes, ruthenium(II) [(6-p-cymene)RuCl(py2CO)]PF6 (1), iridium(III) [(5-Cp)IrCl(py2CO)]PF6 (2), and NH4[IrCl4(py2CO)]H2O (3), based on di-2-pyridylketone (py2CO). The prepared...
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Entangled rendezvous: a possible application of Bell non-locality for mobile agents on networks
PublicationRendezvous is an old problem of assuring that two or more parties, initially separated, not knowing the position of each other, and not allowed to communicate, are striving to meet without pre-agreement on the meeting point. This problem has been extensively studied in classical computer science and has vivid importance to modern and future applications. Quantum non-locality, like Bell inequality violation, has shown that in many...
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UK travel agents’ evaluation of eLearning courses offered by destinations: an exploratory study.
PublicationThis study aims to develop an understanding of the use of e-learning courses created for travel agents by Destination Management Organizations (DMOs). It explores agents’ perceptions of such courses. The research examines the views of 304 UK-based travel agents using online survey and investigates whether age, sex, type of agency, work experience, and educational level have influence on e-learning uptake. The satisfaction of travel...
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Phase I and phase II metabolism simulation of antitumor-active 2-hydroxyacridinone with electrochemistry coupled on-line with mass spectrometry.
PublicationHere, we report the metabolic profile and the results of associated metabolic studies of 2-hydroxyacridinone (2-OH-AC), the reference compound for antitumor-active imidazo- and triazoloacridinones. Electrochemistry coupled with mass spectrometry was applied to simulate the general oxidative metabolism of 2-OH-AC for the first time. The reactivity of 2-OH-AC products to biomolecules was also examined. The usefulness of the electrochemistry...
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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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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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Antitumor triazoloacridinone C-1305 as a potent FLT3 tyrosine kinase inhibitor in human acute myeloid leukemia (AML) cells.
PublicationJednym z defektów molekularnych u pacjentów z ostrą białaczką szpikową (AML) jest konstytutywna aktywacja receptoroweej kinazy tyrozynowj FLT3.Najczęstszą mutacją genu kodującego FLT3 jest wewnętrzna tandemowa duplikacja ITD we fragmencie okołobłonowym receptora. W pracy zbadano, czy przeciwnowotworowy triazoloakrydon C-1305 może być inhibitorem kinazy tyrozynowej FLT3. Badania przeprowadzono na dwóch liniach komórkowych białaczek...
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Antitumor DNA-Damaging C-1748 is a New Inhibitor of Autophagy that Triggers Apoptosis in Human Pancreatic Cancer Cell Lines
PublicationDespite the enormous progress that has been made over the past decades in diagnosis, treatment and prevention of many types of tumors, survival rates in pancreatic cancer still remain poor. Pancreatic cancer is one of the most malignant and chemoresistant tumors and the profound mechanism supporting these phenomena is the constitutively activated prosurvival autophagy. The antitumor 1-nitroacridine derivative C-1748 belongs to...
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Prospective study of brentuximab vedotin in relapsed/refractory Hodgkin lymphoma patients who are not suitable for stem cell transplant or multi-agent chemotherapy
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CYP3A4 overexpression enhances apoptosis induced by anticancer agent imidazoacridinone C-1311, but does not change the metabolism of C-1311 in CHO cells
PublicationWe examine whether CYP3A4 overexpression influences the rate and pattern of antitumor imidazoacridinone C-1311 metabolism, in relation to the impact of this overexpression on cell cycle progression and final cellular response of CHO cells following C-1311 treatment. Methods: Three CHO cell lines: CHO-WT, wild type, CHO-HR, overexpressing cytochrome P450 reductase (CPR) and CHO-HR-3A4, coexpressing CPR and CYP3A4 were applied....
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Anthrapyridones, a novel group of antitumour non-cross resistant anthraqui-none analogues. Synthesis and molecular basis of the cytotoxic activity towards K562/DOX cells
PublicationOpracowano syntezę nowej grupy związków z grupy antrapirydonów z odpowiednimi hydrofobowymi lub hydrofilowymi podstawnikami. Badano działanie tych związków na komórkach K562/S i K562/DOX (nadekspresja P-glikoproteiny). Stwierdzono, że zwiększenie lipofilowości zwiększa szybkość P-gp zależnego efluksu z komórki.
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Current state of a dual behaviour of antimicrobial peptides-Therapeutic agents and promising delivery vectors
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The use of eLearning strategies among travel agents in the United Kingdom, India and New Zealand
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Tackling Alzheimer's disease: Hypothetical synergism between anti-inflammatory and anti-diabetic agents
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Structural Characterization and in Vivo Evaluation of β-Hairpin Peptidomimetics as Specific CXCR4 Imaging Agents
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New Class of Antimicrobial Agents: SBA-15 Silica Containing Anchored Copper Ions
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Fermented juices as reducing and capping agents for the biosynthesis of size-defined spherical gold nanoparticles
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High resolution model for assessment of contamination by chemical warfare agents dumped in the Baltic Sea
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Effect of glycols used as glycolysis agents on chemical structure and thermal stability of produced glycolysates
PublicationZaprezentowano warunki glikolizy poliuretanowych odpadów piankowych, przy użyciu różnych glikoli oraz wyniki badań budowy chemicznej glikolizatów oraz ich właściwości termicznych.
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Scalable Maintenance of Address Mapping and Autodetecion in Environments Where Agents are Uncapable of Self-Registration
PublicationWhen working with multi-agent systems it is often desirable to manage the agent set. The existing methods of central monitoring stems from two different fields of application. The first has its roots in in computer network monitoring, the other in mutli-agent simulation environments. Both approaches are not general enough to cater for loosely controlled environments, where the total agent population is not known and often fluctuating,...
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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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Selected anionic and cationic surface active agents determined in river sediments – the Klodnica catchment
PublicationSurface active agents (SAAs) are specific compounds that contain hydrophilic/ hydrophobic group in their molecules named as amphiphilic structures. According to charge on the hydrophilic part of surfactants they can be classified into three main groups: anionic, cationic and non-ionic compounds. Due to the amphiphilic structure of SAAs they have specific properties (e.g. ability to adsorption at different surfaces, reduction of...
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Bee Products and Essential Oils as Alternative Agents for Treatment of Infections Caused by S. aureus
PublicationBacteria of the genus Staphylococcus are important human and veterinary pathogens. A crucial characteristic for this group of bacteria is that they can easily acquire mechanisms of antibiotic resistance for a plethora of antibiotics currently in use for human and animal therapies. Therefore, there is a great need to find novel, non-antibiotic chemotherapeutics with marked antistaphylococcal activity. Promising but still underestimated...
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Travel agents and destination management organizations: eLearning as a strategy to train tourism trade partners.
PublicationThis article offers an overview of the existing online courses run by national destination management organizations (DMOs) in order to better equip travel agents and tour operators in the sales activities of the tourism destinations. These online courses represent one of the B2B offers by DMOs and an interesting opportunity for travel agents, who are trying to find their identity and competitive advantage within the context of...
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Collision-Free Network Exploration
PublicationA set of mobile agents is placed at different nodes of a n-node network. The agents synchronously move along the network edges in a collision-free way, i.e., in no round may two agents occupy the same node. In each round, an agent may choose to stay at its currently occupied node or to move to one of its neighbors. An agent has no knowledge of the number and initial positions of other agents. We are looking for the shortest possible...
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Old Problems - New Solutions: Conversion of Capitals as a Tool for Shaping the Competitive Position in the Economic Field
PublicationThe acts and operations any social actor effectuates in each of the logically distinguished spheres of reality are conditioned by many factors, among which a reliable analysis of the strengths and weaknesses of an agent should be considered of utmost importance. The concept of capitals presented in this article divides the quantity of resources available to all acting agents into four main categories (which allows for determining...
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Old Problems - New Solutions: Conversion of Capitals as a Tool for Shaping the Competitive Position in the Economic Field
PublicationThe acts and operations any social actor effectuates in each of the logically distinguished spheres of reality are conditioned by many factors, among which a reliable analysis of the strengths and weaknesses of an agent should be considered of utmost importance. The concept of capitals presented in this article divides the quantity of resources available to all acting agents into four main categories (which allows for determining...
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Genotoxic effects of antitumor 1-nitroacridines C-857 and its novel analoque 4-methyl-1-nitroacridine C-1748
Publication4-podstawione 1-nitroakrydyny reprezentują nową grupę pochodnych akrydyny zsyntetyzowanych na Politechnice Gdańskiej. W przeprowadzonych badaniach nad pochodnymi C-1748 i C-857 zastosowano dwie metody badawcze: test kometowy oraz zmodyfikowany test mikrojąderkowy (CBMN assay). W teście kometowym wykazano wzrost uszkodzeń DNA w zależności od czasu i stężenia badanych pochodnych 1-nitroakrydyny. Badania aberracji chromosomalnych...
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Acid–Base Equilibrium and Self-Association in Relation to High Antitumor Activity of Selected Unsymmetrical Bisacridines Established by Extensive Chemometric Analysis
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Induction of unique structural changes in guanine-rich DNA regions by the triazoloacridone C-1305, a topoisomerase II inhibitor with antitumor activities.
PublicationCelem pracy było scharakteryzowanie odziaływania związku C-1305 z DNA w porównaniu do innych inhibitorów topoizomerazy II. Badania pokazują, że C-1305 odziaływuje preferencyjnie z parami CG, interkaluje do DNA i zaburza sąsiednie otoczenie w bardzo charakterystyczny sposób, który nie został zaobserwowany u pozostałych 22 badanych związków.
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Increased susceptibility of PARP-1 KO cells to antitumor triazoloacridone C-1305 is associated with permanent G2 cell cycle arrest.
PublicationTriazoloakrydon C-1305 jest nowym inhibitorem topoizomerazy II wykazującym wysoką aktywność przeciwnowotworową. W tej pracy badaliśmy działanie cytotoksyczne pochodnej C-1305 i jej analogu strukturalnego C-1533 wobec komórek fibroblastów mysich i dwóch mutantów, w których uszkodzono gen PARP-1. Jak wykazaliśmy, komórki z uszkodzonym genem PARP-1 są nadwrażliwe na działanie związku C-1305 w porównaniu z komórkami PARP-1 +/+ podczas...
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Acid–Base Equilibrium and Self-Association in Relation to High Antitumor Activity of Selected Unsymmetrical Bisacridines Established by Extensive Chemometric Analysis
PublicationUnsymmetrical bisacridines (UAs) represent a novel class of anticancer agents previously synthesized by our group. Our recent studies have demonstrated their high antitumor potential against multiple cancer cell lines and human tumor xenografts in nude mice. At the cellular level, these compounds affected 3D cancer spheroid growth and their cellular uptake was selectively modulated by quantum dots. UAs were shown to undergo metabolic...
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C421 allele-specific ABCG2 gene amplification confers resistance to the antitumor triazoloacridone C-1305 in human lung cancer cells
PublicationGen ABCG2 charakteryzuje polimorficzność pozycji C341, która jest związana ze znacznym obniżeniem ekspresji tego genu i zdolności do transportu przez błonę komórkową. W pracy wykazaliśmy, że komórki raka płuc, które nabyły oporności na związek C-1305, zmieniły fenotyp z heterozygotycznego w odniesieniu do genu ABCG2 i wykazują amplifikację jedynie allelu C341 genu oraz zwiększoną zawartość mRNA i zmutowanego białka pompy ABCG2...
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Antitumor 1-nitroacridine derivative C-1748, induces apoptosis, necrosis or senescence in human colon carcinoma HCT8 and HT29 cells.
PublicationC-1748 jest związkiem oddziaływującym z DNA i potencjalnym związkiem przeciwnowotworowym szczególnie wobec nowotworów prostaty i jelita grubego przeszczepialnych na myszach.W pracy badano odpowiedź komórek nowotworowych HCT8 i HT29 na działanie pochodnej C-1748, w stężeniach biologicznie istotnych (EC90). Analiza cyklu komórkowego linii HCT8 pokazała, że związek powoduje wzrost frakcji sub-G1, świadczący o apoptozie tych komórek...
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The antitumor compound triazoloacridinone C-1305 inhibits FLT3 kinase activity and potentiates apoptosis in mutant FLT3-ITD leukemia cells.
PublicationAim: FMS-like receptor tyrosine kinase (FLT3) is expressed in some normal hematopoietic cell types and plays an important role in the pathogenesis of acute myeloid leukemia (AML). In this study, we examined the effects of triazoloacridinone C-1305, an antitumor compound, on AML cells with different FLT3 status in vitro. Methods: A panel of human leukemic cell lines with different FLT3 status was used, including FLT3 internal tandem...
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Study of Bioreductive Anticancer Agent RH-1-Induced Signals Leading the Wild-Type p53-Bearing Lung Cancer A549 Cells to Apoptosis
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Natural Products Counteracting Cardiotoxicity during Cancer Chemotherapy: The Special Case of Doxorubicin, a Comprehensive Review
PublicationCardiotoxicity is a frequent undesirable phenomenon observed during oncological treatment that limits the therapeutic dose of antitumor drugs and thus may decrease the effec-‐‑ tiveness of cancer eradication. Almost all antitumor drugs exhibit toxic properties towards cardiac muscle. One of the underlying causes of cardiotoxicity is stimulation of oxidative...
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Solid phase microextraction combined with chromatography - a powerful tool for determination of warfare agents and related compounds
PublicationOpisano zastosowanie mikroekstrakcji do fazy stacjonarnej do izolacji wzbogacania środków bojowych i produktów ich degradacji w powietrzu, wodzie i glebie oraz próbkach bilogicznych. Na etapie oznaczeń końcowych stosuje się najczęściej chromatografię gazową. Anality można pobierać przez bezpośrednie zanurzenie włókna w próbce ciekłej i gazowej oraz w fazie nadpowierzchniowej. Stosując SPME-GC można osiągnąć niskie granice oznaczalności...
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Fixed-Dose Combination of NSAIDs and Spasmolytic Agents in the Treatment of Different Types of Pain—A Practical Review
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Complexing and Chelating Agents Immobilized on Silica Gel and Related Materials and Their Application for Sorption of Inorganic Species
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One-Step Synthesis of W/O and O/W Emulsifiers in the Presence of Surface Active Agents
PublicationThe main goal of this study was to describe the method of the synthesis of the dodecyl-, tetradecyl-, hexadecyl- and octadecyl-propylene glycol emulsifiers in the presence of selected anionic and nonionic surfactants. Acyl propylene glycol emulsifiers were produced by esterification of propane-1,2-diol (propylene glycol, PG) with C12:0-C18:0 fatty acids in the presence of anionic sodium dodecyl sulfate (SDS) and nonionic-poly(ethylene...
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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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Bacterial cellulose vs. bacterial cellulose nanocrystals as stabilizer agents for O/W pickering emulsions
PublicationThe growing interest in Pickering emulsions in functional food systems resulted in the need to find suitable stabilizers for them. The work considers the use of bacterial cellulose for this purpose, and its aim was to compare the properties of disintegrated bacterial cellulose, before and after freeze-drying, and its nanocrystals obtained using H2SO4 under variable of time and concentration conditions. The structure of nanocrystals...
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Distributed Evacuation in Graphs with Multiple Exits
PublicationWe consider the problem of efficient evacuation using multiple exits. We formulate this problem as a discrete problem on graphs where mobile agents located in distinct nodes of a given graph must quickly reach one of multiple possible exit nodes, while avoiding congestion and bottlenecks. Each node of the graph has the capacity of holding at most one agent at each time step. Thus, the agents must choose their movements strategy...
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Quantum dots conjugates with unsymmetrical bisacridines enhance cytotoxicity of these antitumor compounds in lung cancer cells and have protecting effects on normal cells
PublicationBackground: In recent years, with the rapid development of nanotechnology and its extensive applications in the medicine, nanocarriers for anticancer drug delivery have gained a great importance. Spherical semiconductor nanocrystals, frequently called quantum dots (QDs) are very attractive nanomaterials for bioimaging applications and they possess properties as potential candidates for drug carrier. Unsymmetrical bisacridines (UAs),...
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The increased level of cytochrome P450 isoenzyme CYP3A4 affects the cellular response in CHO cells upon antitumor imidazoacridinone C-1311 treatment
PublicationPochodna C-1311 to potencjalny związek przeciwnowotworowy, który dotarł do II fazy badań klinicznych. Związek ten ulega metabolicznej transformacji pod wpływem szczurzych i ludzkich białek mikrosomalnych. Wykazano, że białka cytochromu P450 odpowiadają za przemiany metaboliczne C-1311 jedynie w niewielkim stopniu. Z drugiej strony wykazano, że pochodna C-1311 jest inhibitorem białek cytochromu P450, zwłaszcza izoenzymu CYP1A2...
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Consolidating logs in varying formats into a structured repository = konsolidacja logów w zmiennych formatach do strukturalnego repozytorium
PublicationDuring multi-agent systems development, testing and re- search, possibly voluminous logs are created at distributed agent loca-tions. These logs describe individual agents behavior and state changes. To get the complete picture of the multi-agent system working, it is necessary to consolidate these logs and to store them in a format appropriate for diverse analyzes. Specic issues arise during consolidation if the log formats are...
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Phthalocyanine Derivatives Possessing 2-(Morpholin-4-yl)ethoxy Groups As Potential Agents for Photodynamic Therapy
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The Setting Time of Polyether Impression Materials after Contact with Conventional and Experimental Gingival Margin Displacement Agents
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