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Search results for: DRUGS UNDERELECTROCHEMICAL TRANSFORMATIONS
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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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Barcelona - from the province to Metropolis.The cogent strategy of branding the city
PublicationThe phenomenon of rebranding Barcelona's image, called the Barcelona effect or 'Barcelona Model', is exampled as one of the most spectacular transformations of the city perception in the last decade. Why has Barcelona been successful? Is it the effect of the recently intensified revitalization practice, or has the city of Barcelona built its brand market value for years? The aim of the research is to name these transition...
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Przestrzeń publiczna a przemiany miasta
PublicationPraca składa się z dwunastu rozdziałów. Pierwsza część ma charakter wprowadzający do problematyki przestrzeni publicznej. W rozdziale drugim autorka przywołuje wybrane i ważne dla przedmiotu badań koncepcje teoretyczne oparte na modelu wieloparadygmatycznym. Rozdział trzeci osnuty jest wokół antycznego wzorca przestrzeni publicznej, który ze względu na niezwykłe bogactwo rozwiązań w tym zakresie wywodzi się właśnie z tego pnia....
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Error analysis of calculating average d-q current components using Regular Sampling and Park transformation in FOC drives
PublicationIn electric drives using voltage source inverters, motor currents contain ripple component resulting from pulse-width modulated (PWM) voltage. The frequency range of the ripples is much higher than the bandwidth of current control. Therefore the control is performed on the basis of a fundamental current component, i.e. average value with the averaging time being the PWM period. In majority of cases the average current is measured...
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Detection and time/frequency analysis of electric fields in the ground
PublicationThis paper sets out to detect and characterize electric fields in the ground (such as stray current fields) using a tandem time/frequency method of signal analysis. Results were obtained from investigations performed in the presence of a generated electric field with controlled variable characteristics, and in the presence of an electric field generated by a tramline. The analysis of measurement registers was performed using Short‐Time...
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Feedback Control of Doubly-Fed Generator Connected to Current Source Converter
PublicationDoubly-fed induction generator (DFIG) system supplied by current source converter (CSC) is considered in this article. The DFIG can work in two independent modes: AC grid connection and stand-alone mode. The DFIG is connected to the ac grid directly through its stator and the CSC links the rotor side. In this mode, the active and reactive powers of the DFIG must be controlled. This article proposes two control system structures...
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A Robust Random Forest Model for Classifying the Severity of Partial Discharges in Dielectrics
PublicationPartial Discharges (PDs) are a common source of degradation in electrical assets. It is essential that the extent of the deterioration level of insulating medium is correctly identified, to optimize maintenance schedules and prevent abrupt power outages. Temporal PD signals received from damaged insulation, collected through the IEC-60270 method is the gold standard for PD detection. Temporal signals may be transformed to the frequency...
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Graph Neural Networks and Structural Information on Ionic Liquids: A Cheminformatics Study on Molecular Physicochemical Property Prediction
PublicationIonic liquids (ILs) provide a promising solution in many industrial applications, such as solvents, absorbents, electrolytes, catalysts, lubricants, and many others. However, due to the enormous variety of their structures, uncovering or designing those with optimal attributes requires expensive and exhaustive simulations and experiments. For these reasons, searching for an efficient theoretical tool for finding the relationship...
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Significant Production of Thermal Energy in Partially Ionized Hyperbolic Tangent Material Based on Ternary Hybrid Nanomaterials
PublicationNanoparticles are frequently used to enhance the thermal performance of numerous materials. This study has many practical applications for activities that have to minimize losses of energy due to several impacts. This study investigates the inclusion of ternary hybrid nanoparticles in a partially ionized hyperbolic tangent liquid passed over a stretched melting surface. The fluid motion equation is presented by considering the...
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Cu-HKUST-1 and Hydroxyapatite–The Interface of Two Worlds toward the Design of Functional Materials Dedicated to Bone Tissue Regeneration
PublicationA novel composite based on biocompatible hydroxyapatite (HA) nanoparticles and Cu-HKUST-1 (Cu-HKUST-1@HA) has been prepared following a layer-by-layer strategy. Cu-HKUST-1 was carefully selected from a group of four Cu-based metal−organic frameworks as the material with the most promising antimicrobial activity. The formation of a colloidal Cu- HKUST-1 layer on HA nanoparticles was confirmed by various techniques, e.g., infrared...
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The Spatial Structure of Suburban Zones in Selected Entrepreneurship Nets of the Tricity Metropolitan Area
PublicationThe chapter describes spatial structures and forms of Polish suburban zones shown on the example of two selected towns in the Trojmiasto Metropolitan Area (TMA). The description of the spatial characteristics in the urban sprawl, with focus on the entrepreneurships nests is illustrated by the choice of typological features, such as: form, land use, density. Suburbanisation is described to be global, however one can observe individual...
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Electromagnetic Control and Dynamics of Generalized Burgers’ Nanoliquid Flow Containing Motile Microorganisms with Cattaneo–Christov Relations: Galerkin Finite Element Mechanism
PublicationIn our research work, we have developed a model describing the characteristics of the bio-convection and moving microorganisms in the flows of a magnetized generalized Burgers’ nanoliquid with Fourier’s and Fick’s laws in a stretchable sheet. Considerations have been made to Cattaneo–Christov mass and heat diffusion theory. According to the Cattaneo–Christov relation, the Buongiorno phenomenon for the motion of a nanoliquid in...
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Shrinking-shifting and amplifying-shifting device using transformation optics
PublicationBased on transformation optics (TO), this paper uses geometric divisions and linear coordinate transformations to design “shrinking-shifting—and reshaping”, and “amplifying-shifting—and reshaping” devices. The proposed devices can reshape the sizes and locations of the wrapped-objects inside the core-region. The shrinking-shifting device shrinks the larger object into a smaller one and shifts it to different location, whereas the...
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An Analysis of Neural Word Representations for Wikipedia Articles Classification
PublicationOne of the current popular methods of generating word representations is an approach based on the analysis of large document collections with neural networks. It creates so-called word-embeddings that attempt to learn relationships between words and encode this information in the form of a low-dimensional vector. The goal of this paper is to examine the differences between the most popular embedding models and the typical bag-of-words...
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Electrochemical and in silico approaches for liver metabolic oxidation of antitumor-active triazoloacridinone C -1305
Publication5-Dimethylaminopropylamino-8-hydroxytriazoloacridinone (C-1305) is a promising antitumor compound developed in our laboratory. A better understanding of its metabolic transformations is still needed to explain the multidirectional mechanism of pharmacological action of triazoloacridinone derivatives at all. Thus, the aim of the current work was to predict oxidative pathways of C-1305 that would reflect its phase I metabolism. The...
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Distinguishing of cocrystals from simple eutectic mixtures: phenolic acids as potential pharmaceutical coformers
PublicationThe multiparameter model comprising 1D and 2D QSPR/QSAR descriptors was proposed and validated for phenolic acid binary systems. This approach is based on the optimization of regression coefficients for maximization of the percentage of true positives in the pool of systems comprising either simple binary eutectics or cocrystals. The training set consisted of 58 eutectics and 168 cocrystals. The solid dispersions collection used...
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Quinoline-based thiazolyl-hydrazones target cancer cells through autophagy inhibition
PublicationHeterocyclic pharmacophores such as thiazole and quinoline rings have a significant role in medicinal chemistry. They are considered privileged structures since they constitute several Food and Drug Administration (FDA)-approved drugs for cancer treatment. Herein, we report the synthesis, in silico evaluation of the ADMET profiles, and in vitro investigation of the anticancer activity of a series of novel thiazolyl-hydrazones based...
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Self-assembly, stability and conductance of amphotericin B channels: bridging the gap between structure and function
PublicationAmphotericin B (AmB), one of the most powerful but also toxic drugs used to treat systemic mycoses, is believed to selectively permeabilize fungal cell membranes to ions in a sterol-dependent manner. Unfortunately, the structure of the biologically active AmB channels has long eluded researchers, obstructing the design of safer alternatives. Here, we investigate the structural and thermodynamic aspects of channel formation, stability,...
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Właściwości katalityczne i biomedyczne związków zawierających jony rutenu(II) oraz rutenu(III)
PublicationRuthenium complexes appear in scientific publications mainly as catalysts in the olefins metathesis process. In this review, we want to indicate the research niche regarding the use of ruthenium(II) and ruthenium(III) complexes in other catalytic processes, i.e. polymerization or epoxidation of olefins and depolymerization. We would like to combine the catalytic properties of ruthenium(II,III) complex compounds with their biomedical...
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Stable nanoconjugates of transferrin with alloyed quaternary nanocrystals Ag–In–Zn–S as a biological entity for tumor recognition
PublicationOne way to limit the negative effects of anti-tumor drugs on healthy cells is targeted therapy employing functionalized drug carriers. Here we present a biocompatible and stable nanoconjugate of transferrin anchored to Ag-In-Zn-S quantum dots modified with 11-mercaptoundecanoic acid (Tf-QD) as a drug carrier versus typical anticancer drug, doxorubicin. Detailed investigations of Tf-QD nanoconjugates without and with doxorubicin...
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A five-year retrospective study shows increasing rates of antimicrobial drug resistance in Cabo Verde for both Staphylococcus aureus and Escherichia coli
PublicationObjectives Data on baseline drug resistance is important in informing future antimicrobial stewardship programs. So far, no data on the antimicrobial drug resistance of clinical isolates was available for the African archipelago of Cabo Verde. Methods We have performed a retrospective analysis over five-years (2013-17) of the antimicrombial drug susceptibility profiles of clinical isolates in the two main hospitals of Cabo Verde....
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Adam Smith - pięć razy o racjonalności w ekonomii (Z okazji 240 rocznicy ukazania się "Bogactwa Narodów").
PublicationNiniejszy tekst jest syntetyczną próbą, próbą wykraczającą poza ramy samej ekonomii i wkraczającą w pole filozofii, socjologii i antropologii, umiejscowienia myśli Adama Smitha w szerszej perspektywie, perspektywie mechanizmów kształtowania się w nowożytności nowego rodzaju społeczeństwa i związanych z tym zmian mentalnych mających odbicie w myśli europejskiej. Ogrom problematyki zawęża temat do fundamentalnego dla ekonomii jako...
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Tomasz Szymański dr inż. arch.
PeopleTomasz Szymanski (Ph.D.) is an architect and an assistant professor at the Faculty of Architecture of the Technical University of Gdansk. Graduated at the Faculty of Architecture of the Technical University of Gdansk. Studies completed with a diploma with honors. Research Interests Dr. Tomasz Szymanski are centered around the issue of industrial heritage, re-use, adaptation and revitalization of industrial buildings and objects...
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Mechanism-based inactivation of human cytochrome P450 1A2 and 3A4 isoenzymes by antitumor triazoloacridinone C-1305.
Publication5-Dimethylaminopropylamino-8-hydroxytriazoloacridinone, C-1305, is a promising antitumor therapeutic agent with high activity against several experimental tumors. It was determined to be a potent and selective inhibitor of liver microsomal and human recombinant cytochrome P450 (CYP) 1A2 and 3A4 isoenzymes. Therefore, C-1305 might modulate the effectiveness of other drugs used in multidrug therapy. The objective of this study was...
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Chiral analysis of chloro intermediates of methylamphetamine by one-dimensional and multidementional NMR and GC/MS
PublicationImpurity profiling and classification of abused drugs using chiral analytical techniques is of particular interest and importance because of the additional information obtained fromthis approach. When these methods are applied to the synthesis of illicitly used substances, they can supply valuable information about the conditions/chemicals used in the synthesis. We have applied GC and NMR methods to the study of intermediates found...
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Cellular Effects of Selected Unsymmetrical Bisacridines on the Multicellular Tumor Spheroids of HCT116 Colon and A549 Lung Cancer Cells in Comparison to Monolayer Cultures
PublicationMulticellular tumor spheroids are a good tool for testing new anticancer drugs, including those that may target cancer stem cells (CSCs), which are responsible for cancer progression, metastasis, and recurrence. Therefore, we applied this model in our studies of highly active antitumor unsymmetrical bisacridines (UAs). We investigated the cellular response induced by UAs in 2D and 3D cultures of HCT116 colon and A549 lung cancer...
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Phytochemical screening and biological evaluation of Greek sage (Salvia fruticosa Mill.) extracts
PublicationThis study explores the influence of extraction solvents on the composition and bioactivity of Salvia fruticosa extracts. Ultrasound-assisted extraction with water, ethanol and their mixtures in variable proportions was used to produce four different extracts. An untargeted UPLC/MS‑based metabolomics was performed to discover metabolites profile variation between the extracts. In the analyzed samples, 2704 features had been detected,...
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Green and sustainable hydrogels based on quaternized chitosan to enhance wound healing
PublicationHydrogel-based biomaterials applied as wound dressings provide the wound with a moist environment, which facilitates tissue regeneration through granulation and re-epithelialization. The inherent flexibility and adjustable architecture of hydrogels enables incorporation of cells, antimicrobial drugs, growth factors, and bioactive compounds, which leads to expediting wound contraction and enhancing the regeneration process. The...
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Antipsychotic drug prescription sequence analysis in relation to death occurrence and cardiometabolic drug usage: A retrospective longitudinal study
PublicationThe potential role of antipsychotics in increasing cardiovascular risk of mortality is still debated. The aim of this study was to assess the death risk associated with sequences of first-generation antipsychotic (FGA) and second-generation antipsychotic (SGA) prescriptions, including clozapine and lithium, and drugs for cardiometabolic diseases. We conducted a retrospective longitudinal analysis involving 84,881 patients who received...
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Examination of epigenetic inhibitor zebularine in treatment of skin wounds in healthy and diabetic mice
PublicationDNA methyltransferase inhibitor zebularine was proven to induce regeneration in the ear pinna in mice. We utilized a dorsal skin wound model to further evaluate this epigenetic inhibitor in wound healing. Full-thickness excisional wounds were made on the dorsum of 2 and 10-month-old healthy BALB/c and 3 and 8-month-old diabetic (db/db) mice, followed by topical or intraperitoneal zebularine delivery. Depending on the strain, age,...
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COVID‐19: A systematic review and update on prevention, diagnosis, and treatment
PublicationSince the rapid onset of the COVID-19 or SARS-CoV-2 pandemic in the world in 2019, extensive studies have been conducted to unveil the behavior and emission pattern of the virus in order to determine the best ways to diagnosis of virus and thereof formulate effective drugs or vaccines to combat the disease. The emergence of novel diagnostic and therapeutic techniques considering the multiplicity of reports from one side and contradictions...
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Investigating the disease- modifying properties of sclerotiorin in Alzheimer's therapy using acetylcholinesterase inhibition
PublicationAlzheimer's disease (AD) is a progressive neurodegenerative disorder caused due to the damage and loss of neurons in specific brain regions. It is the most common form of dementia observed in older people. The symptoms start with memory loss and gradually cause the inability to speak and do day-to-day activities. The cost of caring for those affected individuals is huge and is probably beyond most developing countries capability....
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c-Myc Protein Level Affected by Unsymmetrical Bisacridines Influences Apoptosis and Senescence Induced in HCT116 Colorectal and H460 Lung Cancer Cells
PublicationUnsymmetrical bisacridines (UAs) are highly active antitumor compounds. They contain in their structure the drugs previously synthesized in our Department: C-1311 and C-1748. UAs exhibit different properties than their monomer components. They do not intercalate to dsDNA but stabilize the G-quadruplex structures, particularly those of the MYC and KRAS genes. Since MYC and KRAS are often mutated and constitutively expressed in cancer...
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Study of the anticancer potential of Cd complexes of selenazoyl-hydrazones and their sulfur isosters
PublicationThe biological activity of Cd compounds has been investigated scarce since Cd has been recognized as a human carcinogen. However, the toxicity of cadmium is comparable to the toxicity of noble metals such as Pt and Pd. The paradigm of metal toxicity has been challenged suggesting that metal toxicity is not a constant property, yet it depends on many factors like the presence of appropriate ligands. Studies on anticancer activity...
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The Interaction of Heptakis (2,6-di-O-Methyl)-β-Cyclodextrin with Mianserin Hydrochloride and Its Influence on the Drug Toxicity
PublicationOne tetracyclic antidepressant, mianserin hydrochloride (MIA), has quite significant side effects on a patients’ health. Cyclodextrins, which are most commonly used to reduce the undesirable features of contained drugs within their hydrophobic interior, also have the potential to alter the toxic behavior of the drug. The present paper contains investigations and the characteristics of interaction mechanisms for MIA and the heptakis...
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Polish Suburban Landscape made of Enterpereneurial Tissue
PublicationDwa ostatnie dekady w Polsce to okres ekspansywny rozwój małych przedsiębiorstw i równolegle dynamiczne przekształcenia przestrzeni wokół miasta . Rozwój tych dwóch zjawisk nastąpiło w okresie transformacji gospodarczej po 1989 roku . Głównym celem pracy jest zbadanie poziomu interakcji między procesem suburbanizacji i rozwojem sektora MSP w wybranych podmiejskich obszary, na przykładzie Metropolii Trójmiejskiej.
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Wykorzystanie sztucznych sieci neuronowych do wykrywania i rozpoznawania tablic rejestracyjnych na zdjęciach pojazdów
PublicationW artykule przedstawiono koncepcję algorytmu wykrywania i rozpoznawania tablic rejestracyjnych (AWiRTR) na obrazach cyfrowych pojazdów. Detekcja i lokalizacja tablic rejestracyjnych oraz wyodrębnienie z obrazu tablicy rejestracyjnej poszczególnych znaków odbywa się z wykorzystaniem podstawowych technik przetwarzania obrazu (przekształcenia morfologiczne, wykrywanie krawędzi) jak i podstawowych danych statystycznych obiektów wykrytych...
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FURTHER REMARKS ON THE NEO-CLASSICAL NAVIER-STOKES EQUATIONS
PublicationThe seminal Navier-Stokes equations have been stated yet before creation of principles of thermodynamics and the first and second laws. In the literature there is the common opinion that the Navier-Stokes equations cannot be taken as a thermodynamically correct model of “working fluid” which is able to describe transformation of “ heat” into “work” and vice versa. Therefore, in the paper, a new exposition of thermodynamically...
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Kinetics of Intermetallic Phase Precipitation in Manual Metal Arc Welded Duplex Stainless Steels
PublicationThe article presents the influence of heat treatment on the kinetics of transformations in lean duplex LDX2101 steel and a weld made of standard duplex 2209 material, which was welded by manual metal arc welding. Changes in the microstructure, hardness, and magnetic phase content were analyzed after heat treatment was conducted at a temperature of 800 °C for a period ranging from 15 to 1440 min. Light and scanning microscopy, Vickers...
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Modeling and simulation of blood flow under the influence of radioactive materials having slip with MHD and nonlinear mixed convection
PublicationRadioactive materials are widely in industry, nuclear plants and medical treatments. Scientists and workers in these fields are mostly exposed to such materials, and adverse effects on blood and temperature profiles are observed. In this regard, objective of the current study is to model and simulate blood based nanofluid with three very important radioactive materials, named as Uranium dioxide (UO2), Thorium dioxide (ThO2) and...
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A Series of Novel 3D Coordination Polymers Based on the Quinoline-2,4-dicarboxylate Building Block and Lanthanide(III) Ions—Temperature Dependence Investigations
PublicationA series of novel 3D coordination polymers [Ln2(Qdca)3(H2O)x]yH2O (x = 3 or 4, y = 0–4) assembled from selected lanthanide ions (Ln(III) = Nd, Eu, Tb, and Er) and a non-explored quinoline- 2,4-dicarboxylate building block (Qdca2 = C11H5NO4 2) were prepared under hydrothermal conditions at temperatures of 100, 120, and 150 C. Generally, an increase in synthesis temperature resulted in structural transformations and the formation...
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Scaling scrum with a customized nexus framework: A report from a joint industry‐academia research project
Publicationespite a wide range of scaling frameworks available, large-scale agile transformations are not straightforward undertakings. Few organizations have structures in place that fit the predefined workflows – while once one applies an off-the-shelf framework outside of its prescribed process, guidance quickly runs out. In this paper, we demonstrate how to instantiate a method configuration process using a lightweight experimental approach...
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Thermodynamics aspects of interactions between acridine derivatives and DNA
PublicationDNA is a molecular target for many anticancer and antiviral drugs. Therefore, a clear understanding of the interaction of small molecules with DNA is important in the rational design of ligands that can bind to DNA with high affinity and selectivity. There are several methods to investigate interactions between drug and DNA. Some of them measure changing into DNA structures, such as lengthening and untwisting of helix of DNA. Other...
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Chromatographic behavior of a new hybrid type RP material containing silica bonded 1,3-alternate 25,27-bis-[cyanopropyloxy]-26,28-bis-[3-propyloxy]-calix[4]arene
PublicationA novel 1,3-alternate 25,27-bis-[cyanopropyloxy]-26,28-bis-[3-propyloxy]-calix[4]arene-bonded silica gel stationary phase (CalixPrCN) was prepared and it's structure was confirmed by ATR-FTIR spectroscopy and elemental analysis. The CalixPrCN phase was characterized in terms of their surface coverage, hydrophobic selectivity, aromatic selectivity, shape selectivity, hydrogen bonding capacity, residue metal content, and silanol...
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Inhibiting activity of HIV-1: protease, reverse transcriptase and integrase all together by novel compounds using computational approaches (flexible and rigid docking)
PublicationAcquired immunodeficiency syndrome (AIDS), caused by human immunodeficiency virus type 1 (HIV-1) infection, is one of the most challenging diseases in recent decades. Nevertheless the shortcomings of chemical drugs such as toxicity, lack of curative effects, the search for more potent anti-HIV agents have been focused in our study. In current study, novel scaffold was designed having a benzyl and imidazole in it which are very...
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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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Manganese(III) Promoted Cyclization of N-alkenyl-N-(2-hydroxyethyl) amides to Iso-Oxacepham Potent β-Lactamase Inhibitors
PublicationBackground: β-Lactams are still a subject of interest of organic chemists. The main reason for this interest is due to their application as a chemotherapeutic. β-Lactam antibiotics are still the most commonly used drugs in bacterial infections. Method: Methods using 4-exo-trig radical cyclization leading to β-lactams are an alternative to classical Staudinger`s β-Lactams formation. We prepared N-alkenyl-N-(2-hydroxyethyl)amides...
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Activation of Metabotropic Glutamate Receptor (mGlu2) and Muscarinic Receptors (M1, M4, and M5), Alone or in Combination, and Its Impact on the Acquisition and Retention of Learning in the Morris Water Maze, NMDA Expression and cGMP Synthesis
PublicationThe Morris water maze (MWM) is regarded as one of the most popular tests for detecting spatial memory in rodents. Long-term potentiation and cGMP synthesis seem to be among the crucial factors involved in this type of learning. Muscarinic (M1, M4, and M5 receptors) and metabotropic glutamate (mGlu) receptors are important targets in the search for antipsychotic drugs with the potency to treat cognitive disabilities associated with...
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The Physiological Effects of ASMR on Anxiety
PublicationPurpose: Autonomous Sensory Meridian Response is a novel phenomenon that is very popular these days on Youtube and Reddit to its anti-anxiety effects. As the name suggests, ASMR is a relaxing warm sensation that begins on the scalp and spreads throughout the body. This technique is also known as "brain massage," and it relies on soothing sights and sounds, like whispers and slow movements. Investigating these videos is primarily motivated...
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Pharmaceuticals wastewater treatment via different advanced oxidation processes: Reaction mechanism, operational factors, toxicities, and cost evaluation – A review
PublicationPharmaceuticals comprises different drugs used for treating different infections in human being and animals. The huge quantities of pharmaceuticals used are found to discharge into different water resources and cause different health and environmental problems. The continuous and large-scale discharge of pharmaceuticals increases their persistency which can consequently make them more toxic. The different advanced oxidation processes...