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Thermodynamics and Intermolecular Interactions of Nicotinamide in Neat and Binary Solutions: Experimental Measurements and COSMO-RS Concentration Dependent Reactions Investigations
PublikacjaIn this study, the temperature-dependent solubility of nicotinamide (niacin) was measured in six neat solvents and five aqueous-organic binary mixtures (methanol, 1,4-dioxane, acetonitrile, DMSO and DMF). It was discovered that the selected set of organic solvents offer all sorts of solvent effects, including co-solvent, synergistic, and anti-solvent features, enabling flexible tuning of niacin solubility. In addition, differential...
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Modulation of UDP-glucuronidation by acridinone antitumor agents C-1305 and C-1311 in HepG2 and HT29 cell lines, despite slight impact in noncellular systems.
PublikacjaBackground Among the studied antitumor acridinone derivatives developed in our laboratory, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone (C-1305) and 5-diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311) exhibited cytotoxic and antitumor properties against several cancer types and were selected to be evaluated in preclinical and early-phase clinical trials. In the present work, we investigated the impact of C-1305...
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Gamma oscillations precede interictal epileptiform spikes in the seizure onset zone
PublikacjaOBJECTIVE: To investigate the generation, spectral characteristics, and potential clinical significance of brain activity preceding interictal epileptiform spike discharges (IEDs) recorded with intracranial EEG. METHODS: Seventeen adult patients with drug-resistant temporal lobe epilepsy were implanted with intracranial electrodes as part of their evaluation for epilepsy surgery. IEDs detected on clinical macro- and research microelectrodes...
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Synthesis, physicochemical and theoretical studies on new rhodium and ruthenium dimers. Relationship between structure and cytotoxic activity
PublikacjaTwo dimeric compounds of the general formulae (Et3NH)2[Rh2(μ2-L)4Cl2] (1) (where L = thiophene-2-carboxylate) and [((η6-p-cymene)Ru)2(μ-Cl)3]PF6 (2) have been synthesized using a new method. The unique anionic complex 1 (space group P bca) has octahedral coordination in which the equatorial positions are occupied by the oxygen atoms of four thiophene-2-carboxylates in a paddle wheel fashion. In complex 2 (space group ), each Ru(II)...
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Development and validation of a GC–MS/MS method for the determination of 11 amphetamines and 34 synthetic cathinones in whole blood
PublikacjaPurpose Psychoactive compounds that contain a phenylethylamine structure (such as amphetamine-type stimulants and synthetic cathinones) are one of the major classes of stimulants on the recreational drug market. Approximately 670 new psychoactive substances (NPS) are monitored only in Europe; however, new psychoactive compounds are being developed for illicit trade each year. In this context, the development of new analytical procedures...
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Antitumor Activity of Triazine Mimic Antibiotics for DNA-binding Implications (Impressive Activity in Vitro Against a Variety of Tumor Types in the NCI-60 Screen): NSC 710607 To Fight HCT-116 Human Colon Carcinoma Cell Lines in Vivo Using the Hollow Fiber Assay and Xenograft Mouse Models
PublikacjaPurpose Successful clinical applications of DNA-directed selective cytotoxic agents disrupt the vital replication/transcription processes and ultimately lead to cancer cell death. This study aimed to examine the growth screen of two lead triazine compounds in a number of cell lines and xenografts and to develop anticancer agents with noncovalent binding affinity bringing fewer side effects. Methods The NCI initial hollow...
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Experimental and Theoretical Screening for Green Solvents Improving Sulfamethizole Solubility
PublikacjaSolubility enhancement of poorly soluble active pharmaceutical ingredients is of crucial importance for drug development and processing. Extensive experimental screening is limited due to the vast number of potential solvent combinations. Hence, theoretical models can offer valuable hints for guiding experiments aimed at providing solubility data. In this paper, we explore the possibility of applying quantum-chemistry-derived...
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Human UDP-Glucuronosyltransferases: Effects of altered expression in breast and pancreatic cancer cell lines.
PublikacjaIncreased aerobic glycolysis and de novo lipid biosynthesis are common characteristics of invasive cancers. UDP-glucuronosyltransferases (UGTs) are phase II drug metabolizing enzymes that in normal cells possess the ability to glucuronidate these lipids and speed their excretion; however, de-regulation of these enzymes in cancer cells can lead to an accumulation of bioactive lipids, which further fuels cancer progression. We hypothesize...
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Molecular Recognition in Complexes of TRF Proteins with Telomeric DNA
PublikacjaTelomeres are specialized nucleoprotein assemblies that protect the ends of linear chromosomes. In humans and many other species, telomeres consist of tandem TTAGGG repeats bound by a protein complex known as shelterin that remodels telomeric DNA into a protective loop structure and regulates telomere homeostasis. Shelterin recognizes telomeric repeats through its two major components known as Telomere Repeat-Binding Factors, TRF1...
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Comparative molecular dynamics study of dimeric and monomeric forms of HIV-1 protease in ligand bound and unbound state
PublikacjaHuman immunodeficiency virus type 1 protease (HIV-1 PR) is a viral-encoded enzyme that forms a homodimer. HIV-1 PR is essential for replication and assembly of the virus and inactivation of HIV-1 PR enzyme causes production of immature, noninfectious viral particles and thus HIV-1 PR is an attractive target in anti-AIDS drug design. In our current work, we performed molecular dynamics (MD) calculations (500 ns) for two different...
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Long-Term Stability of Benzodiazepines and Z-Hypnotic Drugs in Blood Samples Stored at Varying Temperatures
PublikacjaBenzodiazepines (BZDs) and Z-drugs are among the most commonly prescribed pharmaceuticals in the world and are considered standard care for various mental illnesses and for treatment of sleeping and anxiety disorders, alcohol withdrawal, muscle spasms and epilepsy. Some BZDs are not allowed as pharmaceuticals in many countries, and they are used as "designer benzodiazepines" (DBZDs). All these compounds are typically screened in...
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Fluconazole resistant Candida auris clinical isolates have increased levels of cell wall chitin and increased susceptibility to a glucosamine-6-phosphate synthase inhibitor
PublikacjaIn 2009 Candida auris was first isolated as fungal pathogen of human disease from ear canal of a patient in Japan. In less than a decade, this pathogen has rapidly spread around the world and has now become a major health challenge that is of particular concern because many strains are resistant to multiple class of antifungal drugs. The lack of available antifungals and rapid increase of this fungal pathogen provides an incentive...
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New Peptide Based Fluconazole Conjugates with Expanded Molecular Targets
PublikacjaInfections of Candida spp. etiology are frequently treated with azole drugs. Among azoles, the most widely used in the clinical scenario remains fluconazole (FLC). Promising results in treatment of dangerous, systemic Candida infections demonstrate the advantages of combined therapies carried out with combinations of at least two different antifungal agents. Here, we report five conjugates composed of covalently linked FLC and...
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Improved degradation of etodolac in the presence of core-shell ZnFe2O4/SiO2/TiO2 magnetic photocatalyst
PublikacjaIn the present study, susceptibility to photocatalytic degradation of etodolac, 1,8-diethyl-1,3,4,9 – tetrahydro pyran - [3,4-b] indole-1-acetic acid, which is a non-steroidal anti-inflammatory drug frequently detected in an aqueous environment, was for the first time investigated. The obtained p-type TiO2-based photocatalyst coupled with zinc ferrite nanoparticles in a core-shell structure improves the separation and recovery...
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Anticancer Properties of Amino Acid and Peptide Derivatives of Mycophenolic Acid
PublikacjaBackground: Although Mycophenolic Acid (MPA) is applied as prodrugs in clinic as an immunosuppressant, it also possesses anticancer activity. MPA acts as Inosine-5’-Monophosphate Dehydrogenase (IMPDH) inhibitor, where the carboxylic group at the end of the side chain interacts with Ser 276 of the enzyme via hydrogen bonds. Therefore, MPA derivatives with other polar groups indicated high inhibition too. On the other hand, potent...
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The effect of boron concentration on the electrical, morphological and optical properties of boron-doped nanocrystalline diamond sheets: Tuning the diamond-on-graphene vertical junction
PublikacjaIn this paper, the effect of boron doping on the electrical, morphological and structural properties of free-standing nanocrystalline diamond sheets (thickness ~ 1 μm) was investigated. For this purpose, we used diamond films delaminated from a mirror-polished tantalum substrate following a microwave plasma-assisted chemical vapor deposition process, each grown with a different [B]/[C] ratio (up to 20,000 ppm) in the gas phase....
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Determination of the minimum inhibitory concentration of C-1311 derivatives (C-1296, C-1410, Compound 1, Compound 1-R8) against Candida strains
Dane BadawczeThe datasets contain the results of determining the minimum inhibitory concentration of imidazoacridinone derivatives against C. albicans ATCC 10231, C. glabrata ATCC 90030, C. krusei ATCC 6258 and C. parapsilosis ATCC 22019 and C. albicans clinical strains by the modified M27-A3 specified by the CLSI.
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Bioactive silica-based drug delivery systems containing doxorubicin hydrochloride: In vitro studies
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Use of Materials Based on Polymeric Silica as Bone-Targeted Drug Delivery Systems for Metronidazole
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Homoisocitrate dehydrogenase from Candida albicans: properties, inhibition, and targeting by an antifungal pro-drug
PublikacjaThe LYS12 gene from Candida albicans, coding for homoisocitrate dehydrogenase was cloned and expressed as a His-tagged protein in Escherichia coli. The purified gene product catalyzes the Mg2+- and K+-dependent oxidative decarboxylation of homoisocitrate to alpha-ketoadipate. The recombinant enzyme demonstrates strict specificity for homoisocitrate. SDS-PAGE of CaHIcDH revealed its molecular mass of 42.6±1 kDa, while in size-exclusion...
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Glucosamine-6-phosphate synthase,a novel target for antifungalagents.Molecular modelling studies in drug design
PublikacjaPraca dotyczy modelowania zarówno samych inhibitorów syntazy glukozamino-6-fosforanu jak i ich oddziaływania z obydwiema domenami tego enzymu. Enzym syntaza glukozamino-6-fosforanu został zaproponowany jako nowy cel molekularny w chemoterapii infekcji grzybowych. Zaprojektowano i zsyntezowano szereg inhibitorów tego enzymu - potencjalnych nowych leków przeciwgrzybowych. Dzięki modelowaniu molekularnemu udało się wyjaśnić mechanizm...
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The modulatory effect of green tea catechin on drug resistance in human ovarian cancer cells
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Acinetobacter baumannii isolated from hospital‐acquired infection: biofilm production and drug susceptibility
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Fulminant hepatic failure in woman with iron and non-steroidal anti-inflammatory drug intoxication
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Drug transporter expression profiling in chemoresistant variants of the A2780 ovarian cancer cell line
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Microneedle‐Based Generation of Microbubbles in Cancer Tumors to Improve Ultrasound‐Assisted Drug Delivery
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New Life of an Old Drug: Caffeine as a Modulator of Antibacterial Activity of Commonly Used Antibiotics
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The Current Use of Mass Spectrometry in Combination with Other Separation Techniques in Drug Discovery Arena
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Silver Nanoparticles as Chlorhexidine and Metronidazole Drug Delivery Platforms: Their Potential Use in Treating Periodontitis
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Drug-Releasing Antibacterial Coating Made from Nano-Hydroxyapatite Using the Sonocoating Method
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Cisplatin filled multiwalled carbon nanotubes – a novel molecular hybrid of anticancer drug container
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Effective Permeability of Multi Air Gap Ferrite Core 3-Phase Medium Frequency Transformer in Isolated DC-DC Converters
PublikacjaThe magnetizing inductance of the medium frequency transformer (MFT) impacts the performance of the isolated dc-dc power converters. The ferrite material is considered for high power transformers but it requires an assembly of type “I” cores resulting in a multi air gap structure of the magnetic core. The authors claim that the multiple air gaps are randomly distributed and that the average air gap length is unpredictable at the...
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Comparative Analysis of Laboratory-Made and Industrial-Made Sewage Sludge Ash: Implications for Effective Management Strategy Development
Publikacjafirst_pageDownload PDFsettingsOrder Article Reprints Open AccessArticle Comparative Analysis of Laboratory-Made and Industrial-Made Sewage Sludge Ash: Implications for Effective Management Strategy Development by Bartłomiej Michał Cieślik 1,*ORCID,Oskar Ronda 1ORCID,Elżbieta Grządka 2ORCID,Jolanta Orzeł 2 andJustyna Płotka-Wasylka 1 1 Department of Analytical Chemistry, Faculty of Chemistry, Gdańsk University of Technology, Gabriela...
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DRUG AND CHEMICAL TOXICOLOGY
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DRUG METABOLISM AND DISPOSITION
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DRUG DEVELOPMENT RESEARCH
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DRUG METABOLISM REVIEWS
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In-situ odd random phase electrochemical impedance spectroscopy study on the electropolymerization of pyrrole on iron in the presence of sodium salicylate – The influence of the monomer concentration
PublikacjaIn this work, the potentiostatic electropolymerization of polypyrrole (PPy) on iron in aqueous solution of sodium salicylate and pyrrole is studied in situ by odd random phase electrochemical impedance spectroscopy (ORP-EIS). The influence of the pyrrole concentration on the electrosynthesis process is investigated. The ORP-EIS technique ensures a reliable analysis of the PPy electrosynthesis on iron by means of an advanced data...
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Electrochemical and photoelectrochemical properties of the interface between titania nanotubes covered by conducting polymer in aqueous by conducting polymer in aqueous electrolytes – The effect of various geometry and electrolytes concentration
PublikacjaIn the present work we show the impact of nanotubes (NTs) geometry of titania utilized as a substrate in organic-inorganic systems acting as a p-n junction on efficient conversion of radiation energy into electrochemical energy. The electrolytic bath composition and electrolysis conditions were controlled in order to obtain TiO2NTs of various geometry as a result of electrochemical oxidation of titanium foil. The electrode material...
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ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES
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ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH
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Expert Opinion On Drug Safety
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American Health and Drug Benefits
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Drug Delivery and Translational Research
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Expert Opinion on Drug Delivery
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Journal of Drug Metabolism & Toxicology
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International Journal of Drug Discovery
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Expert Opinion on Drug Discovery
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FOOD AND DRUG LAW JOURNAL
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Drug Healthcare and Patient Safety
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