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Search results for: CHALCONE
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Antifungal action of the oxathiolone-fused chalcone derivative
PublicationAMG-148, pochodna chalkonu z pierścieniem oksatiolonowym, wykazuje aktywność przeciwgrzybową in vitro wobec szczepów grzybowych patogennych dla człowieka, z wartościami minimalnych stężeń hamujących wzrost mieszczących się w zakresie 1-16 mikrogramów na mililitr, natomiast w wyższych stężeniach związek ten działa grzybobójczo. Obecność głównych białek oporności wielolekowej, Cdr1p, Cgr2p lub Mdr1p nie wpływa znacząco na aktywność...
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Chemosensitization of multidrug resistant Candida albicans by the oxathiolone fused chalcone derivatives
PublicationThree structurally related oxathiolone fused chalcone derivatives appeared effective chemosensitizers, able to restore in part sensitivity to fluconazole of multidrug-resistant C.albicans strains. Compound 21 effectively chemosensitized cells resistant due to the overexpression of the MDR1 gene, compound 6 reduced resistance of cells overexpressing the ABC-type drug transporters CDR1/CDR2 and derivative 18 partially reversed fluconazole...
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New Chalcone Derivatives Containing 2,4-Dichlorobenzenesulfonamide Moiety with Anticancer and Antioxidant Properties
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Influence of S-Oxidation on Cytotoxic Activity of Oxathiole-Fused Chalcones
PublicationSynthesis, 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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New Chalcones Derivatives With Potent Antitumor Activity And Their Metabolism In Vitro
PublicationChalcone derivatives exhibit a broad range of biological activities, with antioxidant and cytotoxic properties among the most studied. Despite numerous reports on chalcones as cytotoxic, and potentially anticancer agents, very little is know on their actual mechanism of activity. Generally, chalcones are considered as antimitotic agents, which interfere with tubulin assembly.We have recently developed a new class of chalcones with...
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Chalcogen bonding interactions in a series of aromatic selenocyanates
PublicationSelenium atoms in aromatic selenocyanates are characterized by the occurrence of two σ-holes, a stronger one in the prolongation of the NC–Se bond and a weaker one in the prolongation of the Ar–Se bond. The crystal structures of several bis(selenocyanato) derivatives, prepared by a method originally developed for ortho bis-substituted derivatives, illustrate very well this difference, with a short NC–Se⋯NC ChB interaction organizing...
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Novel chalcone-derived pyrazoles as potential therapeutic agents for the treatment of non-small cell lung cancer
PublicationLung cancer is considered to account for approximately one-fifth of all malignant tumor-related deaths worldwide and is therefore one of the most lethal malignancies. Pyrazole scaffold possesses a wide range of biological and pharmacological activities, which play important roles in medicinal chemistry. The present study reports the synthesis and in vitro biological characterization of nine pyrazoles derived from chalcones as potential...
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Structural factors affecting affinity of cytotoxic oxathiole-fused chalcones toward tubulin
PublicationSynthesis, in vitro cytotoxic activity, and interaction with tubulin of (E)-1-(6-alkoxybenzo[d][1,3]oxathiol- 5-yl)-3-phenylprop-2-en-1-one derivatives (2) are described. Some of the compounds demonstrated cytotoxic activity at submicromolar concentrations, and the activity could be related to interaction with tubulin at the colchicine binding site. Interaction of selected derivatives with tubulinwas evaluated using molecular modeling,...
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Hydrogen and chalcogen bonds in crystals of chalcogenadiazolecarboxylic acids – competition or cooperation?
PublicationThis article presents crystal structures of chalcogenadiazolecarboxylic acids bearing both a hydrogen and a chalcogen bond donor. The selected molecules varied in the size of the aromatic unit, the chalcogen atom and/or the position of the carboxyl group in the core structure. The most common synthons in their lattice are "R" _"2" ^"2" (8) self-complementary acid dimers or four-membered [Ch···N]2 rings. Supramolecular synthons...
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Synthesis of isomeric, oxathiolone fuded chalcones and comparison of their activity toward various microorganisms and human cancer cell lines
PublicationIzomeryczne oksationolowe sprzężone chalkony otrzymano w wyniku kondensacji odpowiedniego acetylobenzo[1,3]oksatiolo-2-onu z aldehydem benzoesowym w środowisku kwaśnym. Określono aktywność cytotoksyczną otrzymanych związków wobec komórek linii HeLa, przeciwbakteryjną wobec Micrococcus luteus, Staphylococcus aureus, Salmonella typhimurium, Escherichia coli i Proteus vulgaris, przeciwgrzybową wobec Candida albicans i tuberkulostatyczną...
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Topochemical, Single‐Crystal‐to‐Single‐Crystal [2+2] Photocycloadditions Driven by Chalcogen‐Bonding Interactions
PublicationThe face-to-face association of (E)-1,2-di(4-pyridyl)ethylene (bpen) molecules into rectangular motifs stabilized for the first time by chalcogen bonding (ChB) interactions is shown to provide photoreactive systems leading to cyclobutane formation through single-crystal-to-single-crystal [2+2] photodimerizations. The chelating chalcogen bond donors are based on original aromatic, ortho-substituted bis(selenocyanato)benzene derivatives...
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Impact of the anion and chalcogen on the crystal structure and properties of 4,6-dimethyl-2-pyrimido(thio)nium halides
PublicationBy the reaction of urea or thiourea, acetylacetone and hydrogen halide (HF, HBr or HI), we have obtained seven new 4,6-dimethyl-2-pyrimido(thio)nium salts, which were characterized by single-crystal X-ray diffraction, namely, 4,6-dimethyl-2-oxo-2,3-dihydropyrimidin-1-ium bifluoride, C₆H₉N₂O⁺·HF₂⁻ or (dmpH)F₂H, 4,6-dimethyl-2-oxo-2,3-dihydropyrimidin-1-ium bromide, C₆H₉N₂O⁺·Br⁻ or (dmpH)Br, 4,6-dimethyl-2-oxo-2,3-dihydropyrimidin-1-ium...
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Acid-catalysed synthesis of oxathiolone fused chalkones. Comparison of their activity toward various microrganisms and human cancer lines
PublicationOtrzymano podstawione pochodne oksationolowych sprzężonych chalkonów w wyniku kondensacji 4-acetylo-5-metoksy-2-0ksobenz[1,3]oksatiolu z aldehydem benzoesowym w środowisku kwaśnym. Badano właściwości biologiczne otrzymanych związków. Trzy z otrzymanych pochodnych wykazały umiarkowaną aktywność wobec komórek HeLa, dwa były aktywne wobec Micrococcus luteus i Staphylococcus aureus, a jeden wobec Mycobacterium tuberculosis.
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Synthesis of oxathiolone fused chalkones bearing O-aminoalkyl side chain. Comparison of stability of isomeric benzoxathiolones under alkylation reaction conditions
PublicationIzomeryczne oksatiolonowe sprzężone chalkony zawierające O-alkilowe łańcuchy boczne otrzymano w wyniku kondensacji odpowiednich benzoksatiolonów z podstawionymi benzaldehydami. Wyjściowe benzoksatiolony otrzymano w wyniku alkilowania odpowiednich fenoli chlorkami aninoalkilowymi, jednakże reakcja była często komplikowana w wyniku otwarcia pierścienia oksatiolonowego poprzez grupę aminową. Określono aktywność cytotoksyczną i przeciwdrobnoustrojową...
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Cooperativity of Halogen- and Chalcogen-Bonding Interactions in the Self-Assembly of 4‑Iodoethynyl- and 4,7-Bis(iodoethynyl)benzo-2,1,3-chalcogenadiazoles: Crystal Structures, Hirshfeld Surface Analyses, and Crystal Lattice Energy Calculations
PublicationSeveral new 4-iodoethynyl- and 4,7-bis- (iodoethynyl)benzo-2,1,3-chalcogenadiazoles were prepared, and a comprehensive analysis of the most prominent secondary bonding interactions responsible for the crystal self-assembly was performed using X-ray diffraction. The presence of both the iodoethynyl and chalcogenadiazole moieties allows an evaluation of the preference of these molecules to aggregate through either chalcogen- or halogen-bonding...
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Syntheses and Structures of Transition Metal Complexes with Phosphanylphosphinidene Chalcogenide Ligands
PublicationThe reactivity of the phosphanylphosphinidene complex [(DippN)2W(Cl)(η2-P-PtBu2)]− (1) toward chalcogens (Ch = Se, S) was studied. Reactions of stoichiometric amounts of 1 with chalcogens in DME yielded monomeric tungsten complexes with phosphanylphosphinidene chalcogenide ligands of the formula tBu2P−P−Ch (Ch = Se (in 2) and S (in 5)), which can be regarded as products of the addition of a chalcogen atom to a P=W bond in starting...
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Wykorzystanie wiązań niekowalencyjnych do otrzymywania jedno- i dwuskładnikowych struktur supramolekularnych
PublicationPrzedstawiona rozprawa doktorska dotyczy badań nad wykorzystaniem oddziaływań międzycząsteczkowych do projektowania i syntezy uporządkowanych struktur krystalicznych, ze szczególnym uwzględnieniem wiązań halogenowych i chalkogenowych jako stosunkowo nowych i bardzo atrakcyjnych z punktu widzenia inżynierii kryształu. Praca podzielona jest na kilka części. Pierwsza z nich stanowi wstęp teoretyczny obejmujący opis, założenia oraz...
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Synthesis of 3-(2-Alkylthio-4-chloro-5-methylbenzenesulfonyl)-2-(1-phenyl-3-arylprop-2-enylideneamino)guanidine Derivatives with Pro-Apoptotic Activity against Cancer Cells
PublicationThe untypical course of reaction between chalcones and benzenesulfonylaminoguanidines led to the new 3-(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)-2-(1-phenyl-3-arylprop-2- enylideneamino)guanidine derivatives 8–33. The new compounds were tested in vitro for their impact on the growth of breast cancer cells MCF-7, cervical cancer cells HeLa and colon cancer cells HCT-116 by MTT assay. The results revealed that the activity of...
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Effect of Aromatic System Expansion on Crystal Structures of 1,2,5-Thia- and 1,2,5-Selenadiazoles and Their Quaternary Salts: Synthesis, Structure, and Spectroscopic Properties
PublicationRational manipulation of secondary bonding interactions is a crucial factor in the construction of new chalcogenadiazole-based materials. This article reports detailed experimental studies on phenanthro[9,10-c][1,2,5]chalcogenadiazolium and 2,1,3-benzochalcogenadiazolium salts and their precursors. The compounds were synthesized, characterized employing NMR and UV-Vis spectroscopy. TD-DFT calculations were also performed. The influence...
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Substancje pochodzenia roślinnego przeciwdziałające kardiotoksyczności towarzyszącej chemioterapii nowotworów
PublicationPrawie wszystkie leki przeciwnowotworowe stosowane klinicznie wykazują właściwości toksyczne w stosunku do mięśnia sercowego. Kardiotoksyczność występująca podczas chemioterapii przeciwnowotworowej może być czynnikiem limitującym dawkę leku i tym samym decydującym w znacznym stopniu o skuteczności leczenia. Uważa się, że jednym ze zjawisk przyczyniających się do kardiotoksyczności jest stymulacja stresu oksydacyjnego przez leki...
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High gain/bandwidth off‑chip antenna loaded with metamaterial unit‑cell impedance matching circuit for sub‑terahertz near‑field electronic systems
PublicationAn innovative off-chip antenna (OCA) is presented that exhibits high gain and efficiency performance at the terahertz (THz) band and has a wide operational bandwidth. The proposed OCA is implemented on stacked silicon layers and consists of an open circuit meandering line. It is shown that by loading the antenna with an array of subwavelength circular dielectric slots and terminating it with a metamaterial unit cell, its impedance...
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Two years later: Is the SARS-CoV-2 pandemic still having an impact on emergency surgery? An international cross-sectional survey among WSES members
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Correction to: Two years later: Is the SARS-CoV-2 pandemic still having an impact on emergency surgery? An international cross-sectional survey among WSES members
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18th European Symposium on Radiopharmacy and Radiopharmaceuticals
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Surgical site infection after gastrointestinal surgery in high-income, middle-income, and low-income countries: a prospective, international, multicentre cohort study
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Global variation in anastomosis and end colostomy formation following left‐sided colorectal resection
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Pooled analysis of WHO Surgical Safety Checklist use and mortality after emergency laparotomy
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Effects of hospital facilities on patient outcomes after cancer surgery: an international, prospective, observational study
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Global variation in postoperative mortality and complications after cancer surgery: a multicentre, prospective cohort study in 82 countries
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40th EASD Annual Meeting of the European Association for the Study of Diabetes
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