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Metabolic Profiles of New Unsymmetrical Bisacridine Antitumor Agents in Electrochemical and Enzymatic Noncellular Systems and in Tumor Cells
PublicationNew unsymmetrical bisacridines (UAs) demonstrated high activity not only against a set of tumor cell lines but also against human tumor xenografts in nude mice. Representative UA compounds, named C-2028, C-2045 and C-2053, were characterized in respect to their physicochemical properties and the following studies aimed to elucidate the role of metabolic transformations in UAs action. We demonstrated with phase I and phase II enzymes...
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Novel chalcone-derived pyrazoles as potential therapeutic agents for the treatment of non-small cell lung cancer
PublicationLung cancer is considered to account for approximately one-fifth of all malignant tumor-related deaths worldwide and is therefore one of the most lethal malignancies. Pyrazole scaffold possesses a wide range of biological and pharmacological activities, which play important roles in medicinal chemistry. The present study reports the synthesis and in vitro biological characterization of nine pyrazoles derived from chalcones as potential...
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Design of new cholinesterase inhibitors based on phosphorus analogs of tacrine as potential anti-Alzheimer’s disease agents
PublicationBased on the analysis of the determined free binding energy (using the AutoDock Vina 1.1.2 docking program), the most potent cholinesterase inhibitors were selected. Moreover, studies of 3D visualization of the results of molecular modeling led to the identification of potential sites for the interaction of new potential inhibitors with amino acid residues building active sites of investigated cholinesterases.
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Researching Digital Society: Using Data-Mining to Identify Relevant Themes from an Open Access Journal
PublicationOpen Access scholarly literature is scientific output free from economic barriers and copyright restrictions. Using a case study approach, data mining methods and qualitative analysis, the scholarly output and the meta-data of the Open Access eJournal of e-Democracy and Open Government during the time interval 2009–2020 was analysed. Our study was able to identify the most prominent research topics (defined as thematic clusters)...
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Researching Digital Society: Using Data-Mining to Identify Relevant Themes from an Open Access Journal
PublicationOpen Access scholarly literature is scientific output free from economic barriers and copyright restrictions. Using a case study approach, data mining methods and qualitative analysis, the scholarly output and the meta-data of the Open Access eJournal of e-Democracy and Open Government during the time interval 2009–2020 was analysed. Our study was able to identify the most prominent research topics (defined as thematic clusters)...
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Święto Otwartej Nauki w Bibliotece Politechniki Gdańskiej w ramach Open Access Week 2021
PublicationW dniach 25–31 października 2021 roku odbyła się kolejna edycja Open Access Week, imprezy w Polsce znanej jako Tydzień Otwartej Nauki. Biblioteka PG aktywnie włączyła się w promocję tego naukowego święta poprzez organizację webinariów, prezentacji i spotkań.
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Application of theory of semi-Markov processes to determining distribution of probabilistic process of marine accidents resulting from colission of ships
PublicationIn this paper is presented possible application of the theory of semi-Markov processes to elaborating an eight-state model of the process of occurrence of serviceability state and unserviceability states of sea-going ships making critical manoeuvres during their entering and leaving the ports. In the analysis it was taken into account that sea-going ships are in service for a very long time t (t → ∞). The model was elaborated to...
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Political extremism, group membership and personality traits: who accepts violence? / Extremismo político, pertenencia al grupo y rasgos de personalidad: ¿Quién acepta la violencia?
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Determinants and effects of Poland’s road accidents in the context of the 2030 agenda for sustainable development – poviat level analysis for the years 2010-2019
PublicationThe objective of the research was to assess how selected factors influence road safety in Poland’s poviats. To that end, an analysis was conducted of road accident determinants and effects in the poviats in the years 2010-2019. The time horizon fits in with Goal 3.6. of Agenda 2030, which is to halve the number of global deaths and injuries from road traffic accidents by 2020. The article pres-ents the analysis results for the...
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Synthesis of new antrapyridazone derivatives - a novel group of anticancer agents active on a multidrugresistant(MDR) tumor cell lines
PublicationNovel antrapyridazone derivatives were synthesized and biologically evaluated in order tobroaden the data on structure-activity relationship of this class of cytostatics. Recent literaturedata prove that acetamides react better with aryl chlorides. A new approach based onintroduction of other amides form into aromatic ring in Ullmann was tested. This new methodcould give better yields and make purification step more convenient.
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DNA methylation in cancer development, diagnosis and therapy-multiple opportunities for genotoxic agents to act as methylome disruptors or remediators
PublicationThe role of DNA methylation and recently discovered hydroxymethylation in the function of the human epigenome is currently one of the hottest topics in the life sciences. Progress in this field of research has been further accelerated by the discovery that alterations in the methylome are not only associated with key functions of cells and organisms, such as development, differentiation and gene expression, but may underlie a number...
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Absence of 6-Hydroxydopamine in the Rat Brain After Treatment with Stimulants and Other Dopaminergic Agents: A Mass Fragmentographic Study
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N-Substituted piperazine derivatives as potential multitarget agents acting on histamine H3 receptor and cancer resistance proteins
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Silicon polypodands: powerful metal cation complexing agents and solid–liquid phase-transfer catalysts of new generation
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The Bridge of Knowledge – defining and implementing national Open Access policy by Polish universities. Gdansk University of Technology perspective
PublicationThe European Commission states that Open Access to scientific resources funded by the European Union shall facilitate the use of research results financed from the public funds. Moreover, it will cause an increase in the innovative capacity of Europe. The Open Access landscape is determined by several factors such as mandates. The open mandate may be voluntary or mandatory and implemented at the institutional, national or international...
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The hydration of the protein stabilizing agents: trimethylamine-N-oxide, glycine and its N-methylderivatives - the volumetric and compressibility studies
PublicationThe densities at T = (288.15, 293.15, 298.15, 303.15, and 308.15) K and sound velocities at T = 298.15 K have been measured for aqueous solutions of trimethylamine-N-oxide, glycine, N-methylglycine (sarcosine), N,N-dimethylglycine, N,N,N-trimethylglycine (betaine). From these data the apparent molar volumes, VΦ, the apparent molar isentropic compressions, KS,Φ, and the solvation numbers of solutes have been determined. The concentration...
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Electrochemical simulation of metabolic reduction and conjugation reactions of unsymmetrical bisacridine antitumor agents, C-2028 and C-2053
PublicationElectrochemistry (EC) coupled with analysis techniques such as liquid chromatography (LC) and mass spectrometry (MS) has been developed as a powerful tool for drug metabolism simulation. The application of EC in metabolic studies is particularly favourable due to the low matrix contribution compared to in vitro or in vivo biological models. In this paper, the EC(/LC)/MS system was applied to simulate phase I metabolism of the representative...
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(Re)Shaping Open Access Policy to Scientific Resources at Polish Technical Universities: Gdańsk University of Technology Perspective
PublicationDeveloping European Open Access policy to scientific resources is one of the most important issues undertaken during the public debate about future scholarly communication trends. The Open Access landscape is determined by several factors (e.g. mandates). The open mandate: voluntary or mandatory, can be implemented at the institutional, national or international level. It requires scholars to use open repository to deposit results...
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Comparison of Lithuanian and Polish Consonant Phonemes Based on Acoustic Analysis – Preliminary Results
PublicationThe goal of this research is to find a set of acoustic parameters that are related to differences between Polish and Lithuanian language consonants. In order to identify these differences, an acoustic analysis is performed, and the phoneme sounds are described as the vectors of acoustic parameters. Parameters known from the speech domain as well as those from the music information retrieval area are employed. These parameters are...
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Rosuvastatin based novel 3-substituted isocoumarins / 3-alkylidenephthalides: Ultrasound assisted synthesis and identification of new anticancer agents
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Novel molecules containing structural features of NSAIDs and 1,2,3-triazole ring: Design, synthesis and evaluation as potential cytotoxic agents
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Structure modification of acridine antitumor agents results in changes of enzymatic activity and gene expression of CYP3A4 isoenzyme in HepG2 cells.
PublicationEkspresja izoenzymu CYP3A4, który zaangażowany jest w metabolizm ok. 60% leków stosowanych klinicznie, może być modulowana przez takie czynniki jak: polimorfizm, czynniki transkrypcyjne oraz obecność ksenobiotyków. Przykładem induktorów genów kodujących izoenzym CYP3A4 jest fenobarbital i rifampicyna, których obecność w organizmie przyspiesza metabolizm innych leków stosowanych jednocześnie, które są substratami dla CYP3A4. Dlatego...
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Secure access control and information protection mechanisms in radio system for monitoring and acquisition of data from traffic enforcement cameras
PublicationThe study presents the architecture of the Radio System for Monitoring and Acquisition of Data from Traffic Enforcement Cameras (in short: RSMAD), particularly concerning access control and protection of confidential data. RSMAD security structure will be discussed in relation to network security issues. Additionally, the paper presents the results of the work associated with the modelling of potential threats to system security.
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Flexible Films as Anode Materials Based on rGO and TiO2/MnO2 in Li-Ion Batteries Free of Non-Active Agents
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Discovery of phenylselenoether-hydantoin hybrids as ABCB1 efflux pump modulating agents with cytotoxic and antiproliferative actions in resistant T-lymphoma
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Video Cloud Services for Hospitals: Designing an End-to-End Cloud Service Platform for Medical Video Storage and Secure Access
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Making full and immediate Open Access a reality through the repository route – the role of open repositories in implementation of Plan S.
PublicationThesis/Objective: In 2018, research funding institutions associated in cOAlitionS issued PlanS document which aims to accelerate the transition to full and immediate Open Access to publications from publicly funded research until January 2021. Among the recommendations, which mainly relate to publishing in the Open Access model and its financing, there are also guidelines on the implementation of Plan S assumptions through the...
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Anthra[1,2-d][1,2,3]triazine-4,7,12(3H)-triones as a New Class of Antistaphylococcal Agents: Synthesis and Biological Evaluation
PublicationThe development and spread of resistance of human pathogenic bacteria to the action of commonly used antibacterial drugs is one of the key problems in modern medicine. One of the especially dangerous and easily developing antibiotic resistant bacterial species is Staphylococcus aureus. Anthra[1,2-d][1,2,3]triazine-4,7,12(3H)-triones 22–38 have been developed as novel effective antistaphylococcal agents. These compounds have been...
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Novel molecules containing structural features of NSAIDs and 1,2,3-triazole ring: Design, synthesis and evaluation as potential cytotoxic agents
PublicationFor the first time the template containing structural features of more than one NSAIDs and the 1,2,3-triazole ring was explored for the identification of potential cytotoxic agents. These new and complex molecules were predicted to be effective inhibitors of PDE4B by molecular modelling studies in silico. The multi-step synthesis of these compounds were carried out starting from the well-known drug nimesulide and involved the use...
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Towards facts extraction from text in Polish language
PublicationNatural Language Processing (NLP) finds many usages in different fields of endeavor. Many tools exists allowing analysis of English language. For Polish language the situation is different as the language itself is more complicated. In this paper we show differences between NLP of Polish and English language. Existing solutions are presented and TEAMS software for facts extraction is described. The paper shows also evaluation of...
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The role of intestine and liver in glucuronidation of the imidazo- and triazoloacridinone antitumor agents, C-1311 and C-1305: High affinity substrates for UGT1A10
PublicationCelem przeprowadzonych badań było określenie roli poszczególnych izoform UDP-glukuronylotransferazy (UGT)oraz mikrosomów jelita(HIM)i wątroby (HLM) wyizolowanych od różnych pacjentów w metabolizmie pochodnych akrydonu, związków C-1311 i C-1305. Wykazano, że rodziną UGT katalizującą przemiany C-1305 i C-1311 jest UGT1A, z najwyższą aktywnością wykazywaną przez pozawątrobowy izoenzym UGT1A10. Rozkład aktywności frakcji mikrosomalnych...
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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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Effects of Alkaline Cleaning Agents on the Long-Term Performance and Aging of Polyethersulfone Ultrafiltration Membranes Applied for Treatment of Car Wash Wastewater
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Cell Density-Dependent Cytological Stage Profile and Its Application for a Screen of Cytostatic Agents Active Toward Leukemic Stem Cells
PublicationProliferation and expansion of leukemia is driven by leukemic stem cells (LSCs). Multidrug resistance (MDR) of LSCs is one of the main reasons of failure and relapses in acute myeloid leukemia (AML) treatment. In this study, we show that maintaining HL-60 at low cell culture density or applying a 240-day treatment with anthrapyridazone (BS-121) increased the percentage of primitive cells, which include LSCs determining the overall...
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The influence of combination of binding agents on fatigue properties of deep cold in-place recycled mixtures in Indirect Tensile Fatigue Test (ITFT)
PublicationThe publication presents fatigue properties of cold recycled mixtures for eight combinations of binding agents (cement and bituminous emulsion). Cold recycled mixtures were evaluated in Indirect Tensile Fatigue Test (ITFT) at the temperature of 20 C in controlled stress mode. As a function of horizontal stress, fatigue life is strongly influenced by combination of the binding agents. When fatigue life is analyzed as a function...
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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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NADPH-Cytochrome P-450 reductase in strongly involved in activating metabolic transformatios of 9-amino-1-nitroacridine antitumor agents
PublicationCelem pracy było wyjaśnienie roli reduktazy cytochromu P-450 jaką odgrywa ten enzym w przemianach metabolicznych dwóch związków przeciwnowotworowych z grupy pochodnych 1-nitroakrydyny. Zastosowano metodę HPLC do rozdziału metabolitów, a badania struktur przeprowadzono stosując metodę ESI-MS. Wykazano, że badana reduktaza jest zaangażowana bardziej w metabolizm aktywacyjny 1-nitroakrydyn niż metabolizm detoksykacyjny.
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BeesyBees: A mobile agent-based middleware for a reliable and secure execution of service-based workflow applications in BeesyCluster
PublicationIntegrating distributed services into workflows comes with its own set of challenges, including security, coordination, fault tolerance and optimisation of execution time. This paper presents an architecture and implementation - nicknamed BeesyBees - that allows distributed execution of workflow applications in BeesyCluster using agents. BeesyCluster is a middleware that allows users to access distributed resources as well as publish...
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Building Knowledge for the Purpose of Lip Speech Identification
PublicationConsecutive stages of building knowledge for automatic lip speech identification are shown in this study. The main objective is to prepare audio-visual material for phonetic analysis and transcription. First, approximately 260 sentences of natural English were prepared taking into account the frequencies of occurrence of all English phonemes. Five native speakers from different countries read the selected sentences in front of...
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Semantic OLAP with FluentEditor and Ontorion Semantic Excel Toolchain
PublicationSemantic technologies appear as a step on the way to creating systems capable of representing the physical world as real time computational processes. In this context, the paper presents a toolchain for an ontology based knowledge management system. It consists of the ontology editor, FluentEditor and the distributed knowledge representation system, Ontorion. FluentEditor is a comprehensive tool for editing and manipulating complex...
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Acridinone antitumor agents, C-1305 and C-1299 are metabolized rather by flavin-containing monooxygenases and UDP-glucuronosyltransferases than cytochromes P450
PublicationStwierdzono, że to monooksygenazy flawinowe, a nie enzymy cytochromu P450, są głównymi enzymami frakcji mikrosomalnej, odpowiedzialnymi za detoksyfikacyjny metabolizm dwóch badanych pochodnych triazoloakrydonu. Dodatkowo C-1305 ulega sprzęganiu w czasie drugiej fazy metabolizmu z kwasem glukuronowym do postaci O-glukuronidu
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A new pH/organic modifier gradient RP HPLC method for convenient determination of lipophilicity and acidity of drugs as applied to established imidazoline agents
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Synthesis of 7-oxo-7h-naphto[1,2,3-de]quinoline derivatives as potential anticancer agents active on multidrug resistant cell lines
PublicationOpierając się na naszym wcześniejszym stwierdzeniu, że tetracykliczne analogi antrachinonów z wbudowanym pierścieniem pirydynowym wykazują aktywną cytotoksyczność względem komórek z indukowaną opornością, przeprowadzono syntezę pochodnych 7-oxo-7h-nafto[1,2,3-de]chinoliny (3, 6-8, 10-12, 14,15 i 18) posiadających jeden lub dwa zasadowe łańcuchy boczne i różne podstawniki w pierścieniu pirydynowym, związków o potencjalnym działaniu...
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Carbon Dioxide Adsorption over Activated Carbons Produced from Molasses Using H2SO4, H3PO4, HCl, NaOH, and KOH as Activating Agents
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Carbon Dioxide Adsorption Over Activated Carbons Produced from Molasses Using H2so4, H3po4, Hcl, Naoh, and Koh as Activating Agents
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Role of Human UDP-Glucuronosyltransferases in the Biotransformation of the Triazoloacridinone and Imidazoacridinone Antitumor Agents C-1305 and C-1311 : Highly Selective Substrates for UGT1A10
Publication5-Diethylaminoethylamino-8-hydroxyimidazoacridinone, C-1311 (NSC-645809), is an antitumor agent shown to be effective against breast cancer in phase II clinical trials. A similar compound, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone, C-1305, shows high activity against experimental tumors and is expected to have even more beneficial pharmacological properties than C-1311. Previously published studies showed that these...
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Prophylaxis of Non-communicable Diseases: Why Fruits and Vegetables may be Better Chemopreventive Agents than Dietary Supplements Based on Isolated Phytochemicals?
PublicationThe World Health Organization (WHO) report from 2014 documented that non-communicable socalled civilization diseases such as cardiovascular disease, chronic respiratory diseases, cancer or type 2 diabetes are responsible for over 50% of all premature deaths in the world. Research carried out over the past 20 years has provided data suggesting that diet is an essential factor influencing the risk of development of these diseases....
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CYP3A4-dependent cellular response does not relate to CYP3A4-catalysed metabolites of C-1748 and C-1305 acridine antitumor agents in HepG2 cells
PublicationHigh CYP3A4 expression sensitizes tumor cells to certain antitumor agents while for others it can lower their therapeutic ef fi cacy. We have elucidated the in fl uence of CYP3A4 overexpression on the cellular response induced by antitumor acridine derivatives, C-1305 and C-1748, in two hepatocellular carcinoma (HepG2) cell lines, Hep3A4 stably transfected with CYP3A4 isoenzyme, and HepC34 expressing empty vector. The compounds...
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Cancer stem cells in drug resistance and drug screening: can we exploit the cancer stem cell paradigm in search for new antitumor agents?
PublicationPraca przedstawia przegląd literatury dotyczącej hipotezy komórek pierwotnych nowotworu, w szczególności w ich oporności na istniejące terapie. Dyskutowane jest także zagadnienie możliwości wykorzystania wiedzy o tych komórkach do konstrukcji nowych testów do badań przesiewowych in vitro w celu poszukiwania nowych leków przeciwnowotworowych.
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Essential Oils, Silver Nanoparticles and Propolis as Alternative Agents Against Fluconazole Resistant Candida albicans, Candida glabrata and Candida krusei Clinical Isolates
PublicationDevelopment of effective and safe therapeutic treatment of fungal infections remains one of the major challenge for modern medicine. The aim of presented investigation was to analyze the in vitro antifungal activity of selected essential oils, ethanolic extracts of propolis and silver nanoparticles dropped on TiO2 against azole-resistant C. albicans (n = 20), C. glabrata (n = 14) and C. krusei (n = 10) clinical isolates. Among...