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Wyniki wyszukiwania dla: BATRACYLIN ANALOGUES
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Phosphate tricyclic coumarin analogs as steroid sulfatase inhibitors: synthesis and biological activity.
PublikacjaIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate tricyclic coumarin derivatives as potential steroid sulfatase inhibitors. The described synthesis includes the straightforward preparation of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c]chromen-6-one modified...
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Molecular Docking-Based Study of Vasopressin Analogues Modified at Positions 2 and 3 with N-Methylphenylalanine: Influence on Receptor-Bound Conformations and Interactions with Vasopressin and Oxytocin Receptors
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Contribution of UDP-glucuronosyltransferases (UGTs) in metabolism of acridinone antitumor agents, C-1311, C-1305, and their less active structural analogues, C-1330 and C-1299
PublikacjaCelem prowadzonych badań było określenie roli UDP-glukuronylotransferaz, uważanych za najważniejsze enzymy detoksykujące, w metabolizmie pochodnych imidazo- i triazoloakrydonu. Wykazano, że najbardziej aktywne przeciwnowotworowo związki z obu grup, tj. C-1311 i C-1305 są transformowane do O-glukuronidów, w przeciwieństwie do ich metoksylowych analogów, odpowiednio związku C-1330 i C-1299. Analiza składu mieszanin reakcyjnych zawierających...
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Iso-Partricin, an Aromatic Analogue of Amphotericin B: How Shining Light on Old Drugs Might Help Create New Ones
PublikacjaPartricin is a heptaene macrolide antibiotic complex that exhibits exceptional antifungal activity, yet poor selective toxicity, in the pathogen/host system. It consists of two compounds, namely partricin A and B, and both of these molecules incorporate two cis-type bonds within their heptaenic chromophores: 28Z and 30Z. In this contribution, we have proven that partricins are susceptible to a chromophore-straightening photoisomerization...
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Dynamics of hepatitis B virus quasispecies heterogeneity in association with nucleos(t)ide analogue treatment determined by MALDI-TOF MS
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Combined anticancer therapy with imidazoacridinone analogue C‐1305 and paclitaxel in human lung and colon cancer xenografts—Modulation of tumour angiogenesis
PublikacjaThe acridanone derivative 5-dimethylaminopropylamino- 8- hydroxytriazoloacridinone (C-1305) has been described as a potent inhibitor of cancer cell growth. Its mechanism of action in in vitro conditions was attributed, among others, to its ability to bind and stabilize the microtubule network and subsequently exhibit its tumour- suppressive effects in synergy with paclitaxel (PTX). Therefore, the objective of the present study...
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Theoretical conformational analysis of six arginine vasopressin analogs with the l -naphthylalanine in position 3
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The influence of a synthetic growth hormone‐releasing hormone analogue G11 and opioid peptide biphalin on selected fibroblasts parameters relevant to wound healing
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Conformational Studies of [11è12(CN4)]ScyII and [15è16(CN4)]ScyII? Two Scyliorhinin II Analogues by means of 2D NMR Spectroscopy and Theoretical Methods
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Exposure to Bisphenol A Analogs and the Thyroid Function and Volume in Women of Reproductive Age—Cross-Sectional Study
PublikacjaBisphenols (BPs) are commonly known plastifiers that are widely used in industry. The knowledge about the impact of BPs on thyroid function is scarce. Proper thyroid functioning is especially important for women of reproductive age, as hypothyroidism affects fertility, pregnancy outcomes and the offspring. There are no studies analyzing the influence of BPs on thyroid function and volume in non-pregnant young women. The aim of...
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Muramyl dipeptide-based analogs as potential anticancer compounds: Strategies to improve selectivity, biocompatibility, and efficiency
PublikacjaAccording to the WHO, cancer is the second leading cause of death in the world. This is an important global problem and a major challenge for researchers who have been trying to find an effective anticancer therapy. A large number of newly discovered compounds do not exert selective cytotoxic activity against tumorigenic cells and have too many side effects. Therefore, research on muramyl dipeptide (MDP) analogs has attracted interest...
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Synthesis of new polycyclic anthracenodione analogs with hetero- or carbocyclic ring(s) fused to the chromophore system
PublikacjaZsyntezowano serię nowych analogów antracenodionów z różnymi pierścieniami hetero- lub karbocyklicznymi sprzężonymi z układem chromoforowym. Związki te mogą stanowić nową klasę pochodnych antracenodionów o potencjalnej zdolności pokonywania oporności wielolekowej komórek nowotworowych.
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Fluorescent analogs of trypsin inhibitor SFTI-1 isolated from sunflower seeds-synthesis and applications
PublikacjaThis article describes the synthesis and enzymatic study of newly synthesized analogs of trypsin inhibitors SFTI-1 that were fluorescent labeled on their N-terminal amino groups. Two fluorescent derivatives of benzoxazole (3-[2-(4-diphenylaminophenyl) benzoxazol-5-yl]-L-alanine[(4NPh(2)) Ph] Box-Ala and 3-[2-(2', 4', 5'-trimethoxyphenyl) benzoxazol-5-yl]-l-alanine-[2,4,5-(OMe)3Ph] Box-Ala) were used as efficient fluorescent labels....
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Investigation of peptide splicing using two‐peptide‐chain analogs of trypsin inhibitor SFTI‐1
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Genotoxic effects of antitumor 1-nitroacridines C-857 and its novel analoque 4-methyl-1-nitroacridine C-1748
Publikacja4-podstawione 1-nitroakrydyny reprezentują nową grupę pochodnych akrydyny zsyntetyzowanych na Politechnice Gdańskiej. W przeprowadzonych badaniach nad pochodnymi C-1748 i C-857 zastosowano dwie metody badawcze: test kometowy oraz zmodyfikowany test mikrojąderkowy (CBMN assay). W teście kometowym wykazano wzrost uszkodzeń DNA w zależności od czasu i stężenia badanych pochodnych 1-nitroakrydyny. Badania aberracji chromosomalnych...
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Elżbieta Luboch prof. dr hab. inż.
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Antitumor Effects of Vitamin D Analogs on Hamster and Mouse Melanoma Cell Lines in Relation to Melanin Pigmentation
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Inhibitory and antimicrobial activities of OGTI and HV-BBI peptides, fragments and analogs derived from amphibian skin
PublikacjaA series of linear and cyclic fragments and analogs of two peptides (OGTI and HV-BBI) isolated from skin secretions of frogs were synthesized by the solid-phase method. Their inhibitory activity against several serine proteinases: bovine beta-trypsin, bovine alpha-chymotypsin, human leukocyte elastase and cathepsin G from human neutrophils, was investigated together with evaluation of their antimicrobial activities against Gram-negative...
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Design of new cholinesterase inhibitors based on phosphorus analogs of tacrine as potential anti-Alzheimer’s disease agents
PublikacjaBased 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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Cis/trans conformational equilibrium across the N-methylphenylalanine2- N-methylphenylalanine3 peptide bond of arginine vasopressin analogs
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An Influence of the Aromatic Side Chains Conformations in Positions 2 and 3 of Vasopressin Analogs on Interactions with Vasopressin and Oxytocin Receptors
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Application and evaluation of M-EPDG for performance analysis of Polish typical flexible and rigid pavements
PublikacjaThe main goal of the paper is to implement and evaluate the M-EPDG and the software AASHTOware to analyse the performance of new flexible and rigid pavements designed according to the Polish catalogues, which are comparable with analogous catalogues used in other European countries. For this purpose the site-specific inputs for Poland were determined and described in the paper as well as compared to the default input data used...
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Synthetic lipopeptides as potential topical therapeutics in wound and skin care: in vitro studies of permeation and skin cells behaviour
PublikacjaSeveral Gly-His-Lys analogues were obtained to investigate their antimicrobial properties. Three lipophilic analogues with the structure numbering 1b, 2b, 4b, exhibit significant effect against bacteria and were selected for in vitro evaluation of skin cells behaviour. In the present studies, an in vitro model of wound repair, proliferative cell staining, and tracking of living cells were used. Cell proliferation and cell migration,...
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Antiproliferative Activity of Double Point Modified Analogs of 1,25-Dihydroxyvitamin D2 Against Human Malignant Melanoma Cell Lines
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Synthesis, activity on NK-3 tachykinin receptor and conformational solution studies of scyliorhinin II analogs modified at position 16
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Lipidated Analogs of the LL-37-Derived Peptide Fragment KR12—Structural Analysis, Surface-Active Properties and Antimicrobial Activity
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Powder x-ray diffraction pattern of polycrystalline synthetic leningradite, PbCu3V2O8Cl2
Dane BadawczePolycrystalline sample of Cu2+ (S=1/2) antiferromagnetic PbCu3V2O8Cl2 (synthetic analogue of the mineral leningradite) was prepared by solid state reaction of PbCl2, CuO, and V2O5.
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Synthesis of novel dinuclear ruthenium polypyridine dye for dye-sensitized solar cells application
PublikacjaA new dinuclear ruthenium(II) polypyridine complex has been successfully synthesized. The new compound has been characterized by spectroscopic and electrochemical methods. Its potential application as a sensitizing dye in dye-sensitized solar cells has been checked under AM 1.5 G irradiation conditions (100 mW cm−2) and its performance was compared to that of a commercially available mononuclear analogous dye. The overall light-to-electricity...
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Synthesis and antimicrobial activity of truncated fragments and analogs of citropin 1.1: The solution structure of the SDS micelle-bound citropin-like peptides
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Development of potent and effective SARS-CoV-2 main protease inhibitors based on maleimide analogs for the potential treatment of COVID-19
PublikacjaIn the present work, we report a new series of potent SARS-CoV-2 Main Protease (Mpro) inhibitors based on maleimide derivatives. The inhibitory activities were tested in an enzymatic assay using recombinant Mpro (3CL Protease from coronavirus SARS-CoV-2). Within the set of new Mpro inhibitors, 6e demonstrated the highest activity in the enzymatic assay with an IC50 value of 8.52 ± 0.44 mM. The IC50 value for Nirmatrelvir (PF-07321332,...
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Molecular docking studies towards development of novel Gly-Phe analogs for potential inhibition of Cathepsin C (dipeptidyl peptidase I).
PublikacjaCathepsin C is a cysteine protease required for activation of various pro-inflammatory serine proteases and, essentially, is of interest as a therapeutic target. Cathepsin C coordinate system was employed as a model to study the interaction of some already available inhibitors of Cathepsin C. Compounds containing Gly-Phe fragment with functional groups at its ends were designed by knowledge based approach. Using AutoDock and...
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L-Homoserine O-acetyltransferase (CaMet2p) activity and inhibition
Dane BadawczeThe dataset contains the description of methodology and data files with the results obtained spectrophotometrically at 412 nm to determine the rate of fungal enzyme activity. The goal of the study was to obtain conditions optimal for L-homoserine O-acetyltransferase (Met2p) activity as well as evaluation of inhibitory potential of commercially available...
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Bogdan Pankiewicz dr hab. inż.
OsobyBogdan Pankiewicz ukończył w 1993 r. Wydział Elektroniki Politechniki Gdańskiej, specjalność układy elektroniczne a w 2002 r. uzyskał stopień doktora w dziedzinie elektroniki na Wydziale ETI, PG. Od początku kariery jest związany z Politechniką Gdańską: najpierw jako asystent (lata 1994–2002), a następnie jako adiunkt (od 2002 r.) na Wydziale Elektroniki, Telekomunikacji i Informatyki. Zajmuje się projektowaniem analogowych i cyfrowych...
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Antiproliferative activity of side-chain truncated vitamin D analogs (PRI-1203 and PRI-1204) against human malignant melanoma cell lines
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NMR studies of new arginine vasopressin analogs modified with α-2-indanylglycine enantiomers at position 2 bound to sodium dodecyl sulfate micelles
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Opioid Growth Factor and its Derivatives as Potential Non-toxic Multifunctional Anticancer and Analgesic Compounds
PublikacjaIn this paper, we review the structure-activity relationship of OGF and its analogues. We highlight also OGF derivatives with analgesic, immunomodulatory activity and the ability to penetrate the blood-brain barrier and may be used as safe agents enhancing chemotherapy efficacy and improving quality of life in cancer patients. The reviewed papers indicate that Met-enkephalin and its analogues are interesting candidates for the...
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Synteza i aktywność biologiczna koniugatów muramylopeptydów ze związkami o stwierdzonej lub potencjalnej aktywności przeciwnowotworowej i immunostymulacyjnej.
PublikacjaOpisano syntezę nowych połączeń muramylodipeptydu (MDP), nor-muramylo-dipeptydu (nor-MDP), desmuramylopeptydu z aminowymi pochodnymi 1-nitroakrydyny/4-nitroakrydonu, N-(hydroksyalkilo)-4-karboksyamido-akrydyny/9-akrydonu, batracyliną i jej pochodnymi oraz tuftsyną i tuftsyną o odwróconej sekwencji. Zsyntetyzowane związki zostały przekazane do badań biologicznych w National Cancer Institute (NCI, Bethesda, USA) oraz w Katedrze Histologii...
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Distributed Representations Based on Geometric Algebra: the Continuous Model
PublikacjaAuthors revise the concept of a distributed representation of data as well as two previously developed models: Holographic Reduced Representation (HRR) and Binary Spatter Codes (BSC). A Geometric Analogue (GAc - ''c'' stands for continuous as opposed to its discrete version) of HRR is introduced - it employs role-filler binding based on geometric products. Atomic objects are real-valued vectors in n-dimensional Euclidean space...
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Ionic liquids as an effective and eco-friendly medium for synthesis of nitrosubstituted norbornene analogs Ciecze jonowe jako efektywne i przyjazne środowisku medium dla syntezy nitropodstawionych analogów norbornenu
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(4-(Bis(4-Fluorophenyl)Methyl)Piperazin-1-yl)(Cyclohexyl)Methanone Hydrochloride (LDK1229): A New Cannabinoid CB1 Receptor Inverse Agonist from the Class of Benzhydryl Piperazine Analogs
PublikacjaSome inverse agonists of cannabinoid receptor type 1 (CB1) have been demonstrated to be anorectic antiobesity drug candidates. However, the first generation of CB1 inverse agonists, represented by rimonabant (SR141716A), otenabant, and taranabant, are centrally active, with a high level of psychiatric side effects. Hence, the discovery of CB1 inverse agonists with a chemical scaffold distinct from these holds promise for developing...
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Simple and novel synthesis of 3-(thio)phosphoryl-β-lactams by radical cyclization
PublikacjaRadical cyclization of phosphono-acetenamides promoted by manganese(III) acetate leads exclusively to the formation of 3-phosphoryl-β-lactams. The thiophosphoryl analogues were also prepared using this method. In particular, the presented protocol does not require the use of noble metals, while comparable methods do.
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Programmable Input Mode Instrumentation Amplifier Using Multiple Output Current Conveyors
PublikacjaIn this paper a programmable input mode instrumentation amplifier (IA) utilising second generation, multiple output current conveyors and transmission gates is presented. Its main advantage is the ability to choose a voltage or current mode of inputs by setting the voltage of two configuration nodes. The presented IA is prepared as an integrated circuit block to be used alone or as a sub-block in a microcontroller or in a field...
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Experimental and theoretical solubility advantage screening of bi-component solid curcumin formulations
PublikacjaA comprehensive experimental and theoretical screening was performed for identification of curcumin solubilizers. Experimental data led to formulation of a non-linear QSPR model correlating molecular descriptors with measured solubilities. The majority of synthesized binary systems exhibited a moderate enhancement of curcumin solubility, which was found to be the highest in the case of curcumin cocrystallized with pyrogallol. New...
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(CsX)Cu5O2(PO4)2 (X = Cl, Br, I): A Family of Cu2+ S = 1/2 Compounds with Capped-Kagomé Networks Composed of OCu4 Units
PublikacjaThree new salt inclusion compounds (CsX)Cu5O2(PO4)2 (X = Cl, Br, I), phosphate analogues of the kagomé mineral averievite, are reported. Their crystal structures are composed of trigonal networks of corner-sharing OCu4 anion-centered tetrahedra, forming capped-kagomé planes, which can also be regarded as two-dimensional slices along the [111] direction of a pyrochlore lattice. Magnetization and heat capacity measurements reveal...
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Ho2Pd1.3Ge2.7 – a ternary AlB2-type cluster glass system
PublikacjaWe report a successful synthesis of a ternary AlB2-type intermetallic compound. The phase purity was obtained by fine-tuning the Pd-Ge ratio out of the idealized 1-3. Attempts to synthesize an Er analogue were not successful. We discuss the instability of the Er analogue based on the atomic size ratio and also suggest that the increased stability of Ho2Pd1+xGe3−x in the Pd-rich range likely stems from a combination of atomic size...
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Emerging anticancer activity of candidal glucoseamine-6-phosphate synthase inhibitors upon nanoparticle-mediated delivery
PublikacjaNumerous glutamine analogues have been reported as irreversible inhibitors of the glucosamine-6-phosphate (GlcN-6-P) synthase in pathogenic Candida albicans in the last 3.5 decades. Among the reported inhibitors, the most effective N3-(4-methoxyfumaroyl)-L-2,3- diaminopropanoic acid (FMDP) has been extensively studied in order to develop its more active analogues. Several peptide−FMDP conjugates were tested to deliver FMDP to its...
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Analog CMOS processor for early vision processing with highly reduced power consumption
PublikacjaA new approach to an analog ultra-low power visionchip design is presented. The prototype chip performs low-levelconvolutional image processing algorithms in real time. Thecircuit is implemented in 0.35 μm CMOS technology, contains64 x 64 SIMD matrix with embedded analogue processors APE(Analogue Processing Element). The photo-sensitive-matrix is of2.2 μm x 2.2 μm size, giving the density of 877 processors permm2. The matrix dissipates...
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Characteristics of an image sensor with early-vision processing fabricated in standard 0.35 µm CMOS technology
PublikacjaThe article presents measurement results of prototype integrated circuits for acquisition and processing of images in real time. In order to verify a new concept of circuit solutions of analogue image processors, experimental integrated circuits were fabricated. The integrated circuits, designed in a standard 0.35 µm CMOS technology, contain the image sensor and analogue processors that perform low-level convolution-based image...
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New conjugates of tuftsin and muramyl dipeptide as stimulators of human monocytes-derived dendritic cells
PublikacjaMuramyl dipeptide (MDP) and tuftsin are known biologically active compound displaying a significant influence on various cell populations of innate immune response. MDP, as a fragment of bacterial cell wall, stimulates not only macrophages and monocytes, but also dendritic cells. In contrast, little is known about tuftsin influence on these cells. Therefore it seemed vital to access whether tuftsin or its derivatives conjugated...
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Synthesis and Cholinesterase Inhibitory Activity of N-Phosphorylated /N-Tiophosphorylated Tacrine
PublikacjaNovel phosphorus and thiophosphorus tacrine derivatives were designed, synthesized and their biological activity and molecular modeling was investigated as a new potential anti-Alzheimer's disease (AD) agents. All new synthesized compound exhibited lower toxicity against neuroblastoma cell line (SH-SY5Y) in comparison with tacrine. Two analogues in the series, 7 and 9, demonstrated lack of cytotoxicity against hepatocellular cells...