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Wyniki wyszukiwania dla: DRUK%203D
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Smart sustainable cities : Reconnaissance Study
PublikacjaThe global urban population is expected to grow by 63 percent between 2014 and 2050 – compared to an overall global population growth of 32 percent during the same period. Megacities with over 20-million inhabitants will see the fastest increase in population – and at least 13 new megacities are expected by 2030, in addition to the 28 existing today. The fastest growing urban centres contain around one-million inhabitants, and...
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Developing a Metropolitan Transport System—Exemplified by the Gdansk–Gdynia–Sopot Metropolitan Area
PublikacjaAs regional centres with metropolitan functions, metropolises grow and develop depending on how well they can meet the area’s transport needs internally and externally, a result of their socio-economic relations. The transport system of a metropolitan area must ensure that people and goods can move efficiently, effectively and environmentally friendly. Over the last ten years, the transport system of the Gdańsk–Gdynia–Sopot Metropolitan...
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Natural Deep Eutectic Solvents as Agents for Improving Solubility, Stability and Delivery of Curcumin
PublikacjaPurpose Study on curcumin dissolved in natural deep eutectic solvents (NADES) was aimed at exploiting their beneficial properties as drug carriers. Methods The concentration of dissolved curcumin in NADES was measured. Simulated gastrointestinal fluids were used to determine the concentration of curcumin and quantum chemistry computations were performed for clarifying the origin of curcumin solubility enhancement in NADES. Results NADES...
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Phase I and phase II metabolism simulation of antitumor-active 2-hydroxyacridinone with electrochemistry coupled on-line with mass spectrometry.
PublikacjaHere, 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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Organic solvents aggregating and shaping structural folding of protein, a case study of the protease enzyme
PublikacjaLow solubility of reactants or products in aqueous solutions can result in the enzymatic catalytic reactions that can occur in non-aqueous solutions. In current study we investigated aqueous solutions containing different organic solvents / deep eutectic solvents (DESs) that can influence the protease enzyme's activity, structural, and thermal stabilities. Retroviral aspartic protease enzyme is responsible for the cleavage of the...
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The Substantial Improvement of Amphotericin B Selective Toxicity Upon Modification of Mycosamine with Bulky Substituents
PublikacjaAbstract: Background: It is assumed that the unfavorable selective toxicity of an antifungal drug Amphotericin B (AmB) can be improved upon chemical modification of the antibiotic molecule. Objective: The aim of this study was verification of the hypothesis that introduction of bulky substituents at the amino sugar moiety of the antibiotic may result in diminishment of mammalian vitro toxicity of thus prepared AmB derivatives. Methods:...
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Antifungal Activity of Capridine β as a Consequence of Its Biotransformation into Metabolite Affecting Yeast Topoisomerase II Activity
PublikacjaIn the last few years,increasing importance is attached to problems caused by fungal pathogens. Current methods of preventing fungal infections remain unsatisfactory. There are several antifungal compounds whichare highly effective in some cases, however, they have limitations in usage: Nephrotoxicity and other adverse effects. In addition, the frequent use of available fungistatic drugs promotes drug resistance....
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Foliate-Targeting Quantum Dots-β-Cyclodextrin Nanocarrier for Efficient Delivery of Unsymmetrical Bisacridines to Lung and Prostate Cancer Cells
PublikacjaTargeted drug delivery by nanocarriers molecules can increase the efficiency of cancer treatment. One of the targeting ligands is folic acid (FA), which has a high affinity for the folic acid receptors, which are overexpressed in many cancers. Herein, we describe the preparation of the nanoconjugates containing quantum dots (QDs) and β-cyclodextrin (β-CD) with foliate-targeting properties for the delivery of anticancer compound...
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Molecular mechanism of proton-coupled ligand translocation by the bacterial efflux pump EmrE
PublikacjaThe current surge in bacterial multi-drug resistance (MDR) is one of the largest challenges to public health, threatening to render ineffective many therapies we rely on for treatment of serious infections. Understanding different factors that contribute to MDR is hence crucial from the global “one health” perspective. In this contribution, we focus on the prototypical broad-selectivity proton-coupled antiporter EmrE, one of the...
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Imidazoacridinone-dependent lysosomal photodestruction: a pharmacological Trojan horse approach to eradicate multidrug-resistant cancers
PublikacjaMultidrug resistance (MDR) remains a primary hindrance to curative cancer therapy. Thus, introduction of novel strategies to overcome MDR is of paramount therapeutic significance. Sequestration of chemotherapeutics in lysosomes is an established mechanism of drug resistance. Here, we show that MDR cells display a marked increase in lysosome number. We further demonstrate that imidazoacridinones (IAs), which are cytotoxic fluorochromes,...
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Evaluation of possibilities in identification and susceptibility testing for Candida glabrata clinical isolates with the Integral System Yeast Plus (ISYP)
PublikacjaThe aim of this study was to evaluate possibilities of correct identification and susceptibility testing of C. glabrata clinical isolates with Integral System Yeast Plus (ISYP). For species identification, as the reference method, API Candida test and species-specific PCR reactions were used. The potential of antifungal susceptibility testing by the ISYP test was compared with the Sensititre Yeast One. Whilst the reference methods...
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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
PublikacjaHigh 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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Effects of Addictive Substances During Pregnancy and Infancy and Their Analysis in Biological Materials
PublikacjaThe use of addictive substances during pregnancy is a serious social problem, not only because of effects on the health of the woman and child, but also because drug or alcohol dependency it detracts from childcare and enhances the prospect of child neglect and family breakdown. Developing additive substance abuse treatment programs for pregnant women is socially important and can help ensure the health of babies, prevent subsequent...
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Electrochemical simulation of enzymatic transformations studied for the selected antitumor acridine derivatives
PublikacjaThe elucidation of the metabolic pathways and the biotransformation mechanisms of potential drugs is a crucial point in drug development. It allows to know the activation routes of the new biologically active compounds, especially in respect to their possible toxicity. Generally, in vivo or in vitro experiments with liver microsomes or hepatocytes are performed. However, these testing schemes are tedious, time consuming and of...
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Parametric method of preliminary prediction of the ship operating costs.
PublikacjaPraca zawiera rezultaty badań dotyczących parametrycznej metody prognozowania kosztów eksploatacji statku - przydatnej w metodyce projektowania wstępnego okrętów. Przedstawiono założenia koncepcyjne i teoretyczne metody, dokonano identyfikacji czynników istotnie wpływających na koszt eksploatacji statku, z uwzględnieniem czasowej wartości pieniądza. Opracowano wzory służące do wyznaczania składników kosztów eksploatacji statku...
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Tailoring the electrochemical degradation of iron protected with polypyrrole films for biodegradable cardiovascular stents
PublikacjaThe degradation of polypyrrole (PPy) coated iron is studied in phosphate buffer saline solution at 37 °C by odd random phase multisine electrochemical impedance spectroscopy (ORP-EIS). PPy is electropolymerized with anti-inflammatory salicylates incorporated in the film, as a drug release system. The modelling of EIS over time provides the quantitative description of the corrosion behaviour of the material. Thus, the reliable...
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Influence of S-Oxidation on Cytotoxic Activity of Oxathiole-Fused Chalcones
PublikacjaSynthesis, in vitro cytotoxic activity, and interaction with tubulin of oxidized, isomeric 1-(5-alkoxybenzo[d] [1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-ones and 1-(6- alkoxybenzo[d][1,3]oxathiol-5-yl)-3-phenylprop-2-en-1- ones are described. Most of the compounds demonstrated cytotoxic activity at submicromolar concentrations. It was found that oxidation of sulfur atom of the oxathiole-fused chalcones strongly influenced activity...
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Solubility advantage of sulfanilamide and sulfacetamide in natural deep eutectic systems: experimental and theoretical investigations
PublikacjaObjective: The aim of this study was to explore the possibility of using natural deep eutectic solvents (NADES) as solvation media for enhancement of solubility of sulfonamides, as well as gaining some thermodynamic characteristics of the analyzed systems. Significance: Low solubility of many active pharmaceutical ingredients is a well-recognized difficulty in pharmaceutical industry, hence the need for different strategies addressing...
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Synthesis and biological evaluation of N-acylated tyramine sulfamates containing C-F bonds as steroid sulfatase inhibitors
PublikacjaSteroid sulfatase (STS) is responsible for the hydrolysis of biologically inactive sulfated steroids into their active un-sulfated forms and promotes the growth of various hormone-dependent cancers (e.g., breast cancer). Therefore, the STS enzyme is a promising therapeutic target for the treatment of steroid-sensitive cancers. Herein, we report the synthesis and biological evaluation of sulfamate analogs as potential STS inhibitors...
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Synthesis and biological evaluation of fluorinated 3-phenylcoumarin-7-O-sulfamate derivatives as steroid sulfatase inhibitors
PublikacjaIn the present work, we report the initial results of our study on a series of 3-phenylcoumarin sulfamate-based compounds containing C-F bonds as a novel inhibitors of steroid sulfatase (STS). The new compounds are potent STS inhibitors, possessing more than 10 times higher inhibitory potency than coumarin-7-O-sulfamate. In the course of our investigation, compounds 2b and 2c demonstrated the highest inhibitory effect in the enzymatic...
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Simplified, serine‐rich theta‐defensin analogues as antitumour peptides
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CDK9: Therapeutic Perspective in HCC Therapy
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Current Challenges in Targeting Tumor Desmoplasia to Improve the Efficacy of Immunotherapy
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Investigating the disease‐modifying properties of sclerotiorin in Alzheimer's therapy using acetylcholinesterase inhibition
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Current state of a dual behaviour of antimicrobial peptides-Therapeutic agents and promising delivery vectors
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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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Highly Potent Antidiuretic Antagonists: Conformational Studies of Vasopressin Analogues Modified with 1-Naphthylalanine Enantiomers at Position 2
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Structure–activity relationships study on biological activity of peptides as dipeptidyl peptidase IV inhibitors by chemometric modeling
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Design and characteristics of gellan gum beads for modified release of meloxicam
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Aryl- and heteroaryl-substituted phenylalanines as AMPA receptor ligands
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Short Term Monitor of Photodegradation Processes in Ranitidine Hydrochloride Observed by FTIR and ATR FTIR
PublikacjaThe effects of degradation of ranitidine hydrochloride exposed to UVB radiation (l = 310 nm) and oxygen in a weathering chamber were studied by Fourier Transform Infrared spectroscopy (FTIR) and Attenuated Total Reflectance Fourier Transform Infrared spectroscopy (ATR-FTIR). ATR-FTIR profile indicated that the degradation was spatially heterogeneous. Significant amounts of photoproducts were detected only in a directly...
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Effects of an immunosuppressive treatment on the rat prostate
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Novel anticancer strategy aimed at targeting shelterin complexes by the induction of structural changes in telomeric DNA: hitting two birds with one stone.
PublikacjaThe ends of chromosomes in mammals are composed of telomeric DNA containing TTAGGG repeats, which bind specific proteins called shelterins. This telomeric DNA together with shelterins form a cap that protects the ends of chromosomes from being recognized as sites of DNA damage and from chromosomal fusions. Many very successful antitumor drugs used in the treatment of cancer patients bind to DNA, some of them with a prominent sequence...
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Structural Factors Affecting Cytotoxic Activity of (E)-1-(Benzo[d ][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one Derivatives
PublikacjaDerivatives of (E)-1-(5-alkoxybenzo[d][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one (1) demonstrated exceptionally high in vitro cytotoxic activity, with IC50 values of the most active derivatives in the nanomolar range. To identify structural fragments necessary for the activity, several analogs deprived of selected fragments were prepared, and their cytotoxic activity was tested. It was found that the activity depends on combined effects...
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Badania doświadczalne zginanych belek betonowych wykonanych metodą przyrostową w technologii druku 3d.
ProjektyProjekt realizowany w Wydział Inżynierii Lądowej i Środowiska
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Experiences and Challenges in Fatality Reduction on Polish Roads
PublikacjaAccording to the UN, road safety is the key to achieving sustainable development goals, yet the complexity of how road accidents happen makes this a difficult challenge leaving many countries struggling with the problem. For years, Poland has infamously been one of the EU’s top countries for road-accident fatality rates. Despite that, it has made significant progress in the last thirty years with a fatality reduction of more than...
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Comparison of AHP and Numerical Taxonomy Methods Based on Biogas Plant Location Analysis
PublikacjaThe paper presents a comparison of the multi-criteria Analytic Hierarchy Process (AHP) method and numerical taxonomy in biogas plant location selection. Biogas plants are sources that will significantly contribute to the implementation of the provisions of the energy and climate package for Poland by 2030. Increasing the share of energy produced from renewable sources, e.g. biogas plants, will increase the country’s energy security....
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Synthesis and biological activity of ester derivatives of mycophenolic acid and acridines/acridones as potential immunosuppressive agents
PublikacjaImproved 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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Drukowanie trwałych elementów z tworzyw termoplastycznych w technologii FDM/FFF
PublikacjaDrukowanie detali z tworzyw sztucznych stanowi aktualnie jedną z najczęściej wykorzystywanych form druku 3D, która znajduje szerokie zastosowanie zarówno w obszarze amatorskim, jak i również przemysłowym. Omawiane w pracy zagadnienia dotyczą zasady działania oraz charakterystyki najważniejszych czynników technologii FDM/FFF. Przedstawiono najczęściej występujące błędy oraz defekty drukowanych elementów. Wskazano ponadto najważniejsze...
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Lampa nienaftowa - FreeCAD
Kursy OnlineFreeCAD jest uniwersalnym parametrycznym programem modelującym w przestrzeni 3D CAD, którego rozwój odbywa się wyłącznie według zasad Open Source (licencja LGPL) .FreeCAD jest przeznaczony bezpośrednio dla inżynierii mechanicznej i projektowania detali i produktów, ale mieści się również w szerszym zakresie zastosowań związanych z inżynierią, takich jak architektura, analiza elementów ukończonych, druk 3D i wiele pokrewnych. PS Kurs...
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Dietary intervention with beetroot juice during doxorubicin cancer chemotherapy in vivo reduces markers of oxidative stress
PublikacjaCancer chemotherapy with doxorubicin, despite high antitumor activity and broad spectrum of this drug, is on decline due to toxic side effects. The clinical efficacy of anthracyclines have continuously prompted the search for new adjuvants to alleviate undesirable side toxicity incurred by this group of cytostatics. The recent approaches involve the application of synthetic or purified natural antioxidants in combination with doxorubicin...
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Cell Density-Dependent Cytological Stage Profile and Its Application for a Screen of Cytostatic Agents Active Toward Leukemic Stem Cells
PublikacjaProliferation 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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Intermolecular Interactions as a Measure of Dapsone Solubility in Neat Solvents and Binary Solvent Mixtures
PublikacjaDapsone is an effective antibacterial drug used to treat a variety of conditions. However, the aqueous solubility of this drug is limited, as is its permeability. This study expands the available solubility data pool for dapsone by measuring its solubility in several pure organic solvents: N-methyl-2-pyrrolidone (CAS: 872-50-4), dimethyl sulfoxide (CAS: 67-68-5), 4-formylmorpholine (CAS: 4394-85-8), tetraethylene pentamine (CAS:...
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Sustainable polymers targeted at the surgical and otolaryngological applications: Circularity and future
PublikacjaThe ongoing climate changes, high air and noise pollution have significant impact on humans’ health. This influence is especially visible in otolaryngology, which focuses on respiratory and hearing systems disfunctions. However, even though surgeries are done in response to diseases related to climate changes, they also have a negative impact on the environment, mostly connected with the inherence of single-use fossil fuel derived...
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Activation Energy and Inclination Magnetic Dipole Influences on Carreau Nanofluid Flowing via Cylindrical Channel with an Infinite Shearing Rate
PublikacjaThe infinite shear viscosity model of Carreau fluid characterizes the attitude of fluid flow at a very high/very low shear rate. This model has the capacity for interpretation of fluid at both extreme levels, and an inclined magnetic dipole in fluid mechanics has its valuable applications such as magnetic drug engineering, cold treatments to destroy tumors, drug targeting, bio preservation, cryosurgery, astrophysics, reaction kinetics,...
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Docking simulations, Molecular properties and ADMET studies of novel Chromane6,7diol analogues as potential inhibitors of Mushroom tyrosinase
PublikacjaResearch on inhibition of tyrosinase enzyme has attained significant value, because tyrosinase inhibitors have potential applications in medicine, cosmetics (as whitening agents) and in agriculture (as bioinsecticides). Determination and elucidation of new tyrosinase inhibitors are not only beneficial for medical purposes, but their promising applications in improving food quality and nutritional...
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Hel 2019 - video data - pedestrian, bicycles, vehicles
Dane BadawczeHel 2019 - video data - pedestrian, bicycles, vehicles
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Peptydy penetrujące – rodzaje i mechanizmy przenikania przez błony komórkowe
PublikacjaPeptydy penetrujące z pewnością są wyjątkową i ciekawą grupą związków peptydowych. Zostały odkryte ponad dwadzieścia lat temu, ale wiedza na ich temat wciąż jest rozbudowywana. Liczne badania nad mechanizmami ich przenikania do wnętrza komórek pozwalają zrozumieć jakie cechy strukturalne warunkują ich zdolność do penetracji komórek. Wiedza ta pozwala na projektowanie nowych, bardziej efektywnych peptydów penetrujących., które mogą...
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Synthesis, structure characterization and thermal propertiesof [Zr<sub>6</sub>(μ<sub>3</sub>-O)<sub>4</sub>(μ<sub>3</sub>-OH)<sub>4</sub>(OOCCH<sub>2</sub><sup>t</sup>Bu)<sub>9</sub>(μ<sub>2</sub>-OH)<sub>3</sub>]<sub>2</sub>
PublikacjaTytułowy związek otrzymano w reakcji Zr(OiPr)4 z nadmiarem kwasu 3,3-dimetylobutyrowego. Rentgenowska analiza strukturalna została wykonana w temperaturze 103 i 153K. Struktury zawierają dimery podjednostek o wzorze: [Zr6(μ3-O)4(μ3-OH)4-(OOCCH2tBu)9] połączonych 6 mostkującymi grupami μ2-OH. Analiza zmiennotemperaturowych...