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Search results for: indol
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Indo-French Comprehensive Bilateral Cooperation: A Roadmap to Indo-Pacific Parks Partnership and Beyond
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Indo-French Defence and Security Partnership
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India and France bilateral partnership for advancing strategic autonomy in the Indo-Pacific region: Special reference to the Indo-French strategic partnership
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Stereoselective Alkylation of Indole with 5-Arylidene-Meldrum’s Acids in the Presence of Organocatalysts
PublicationBackground: Indole motif is frequently present in biologically active compounds. Enantiomerically pure or enriched 2,2-dimethyl-5-(aryl(1H-indol-3-yl)methyl)-1,3-dioxane-4,6-diones can be considered as a convenient starting point for the synthesis of a indole ring fused with cyclic ketones with biological activity. Preparation of chiral 2,2-dimethyl-5-(aryl(1H-indol-3-yl)methyl)-1,3-dioxane- 4,6-diones requires the reaction of...
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The European Union Strategy for Partnership in the Indo-Pacific Region
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Indo-Iranian Journal
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Indo-European Linguistics
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INDO–FRENCH DEFENCE PARTNERSHIP AND REGIONAL SECURITY BALANCE IN SOUTH ASIA
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Indole-Acrylonitrile Derivatives as Potential Antitumor and Antimicrobial Agents—Synthesis, In Vitro and In Silico Studies
PublicationA series of 2-(1H-indol-2-yl)-3-acrylonitrile derivatives, 2a–x, 3, 4a–b, 5a–d, 6a–b, and 7, were synthesized as potential antitumor and antimicrobial agents. The structures of the prepared compounds were evaluated based on elemental analysis, IR, 1H- and 13NMR, as well as MS spectra. X-ray crystal analysis of the representative 2-(1H-indol-2-yl)-3-acrylonitrile 2l showed that the acrylonitrile double bond was Z-configured. All...
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Synthesis of disubstituted 1,3,4,9-tetrahydropyrano-[3,4-b]indole-1-acetic acids derivatives
Publication1,3,4,9-tetrahydropyrano[3,4-b ]indole-1-acetic acid derivatives are of interest for pharmaceutical research as a core structure for synthesis of biological active substance - Etodolac (selective Cyclooxygenase-2 inhibitor, which belongs to the Non-steroidal Anti-inflammatory Drug, NSAID, that shows a clin-ically effective analgesic and anti-inflammatory activity). Here the way of synthesis of two 1,3,4,9-tetrahydropyrano[3,4-b...
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The Geo-Economics Approach to the European Union Strategic Partnership in the Indo-Pacific Region
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The geo-economic approach to the European Union’s strategy for cooperation in the Indo-Pacific region
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Indo–French Defence Cooperation in the Light of Regional Security Balance in South Asia
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Journal of Indo-European Studies
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Indo-Pacific Journal of Phenomenology
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General, Mild, and Metal-Free Functionalization of Indole and Its Derivatives Through Direct C3-Selenylation
PublicationA very mild method for the introduction of functionalized alkylselenyl group at C-3 position of the indole ring was developed. The proposed procedure consists of an electrophilic substitution of indole and its derivatives with bis(O,O-diisopropoxyphosphorothioyl) diselenide and subsequent cleavage of the P–Se bond with tetrabutylammonium fluoride in the presence of various electrophilic reagents. This method can be successfully...
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Structure-based design and evaluation of novel N-phenyl-1H-indol-2-amine derivatives for fat mass and obesity-associated (FTO) protein inhibition
PublicationFat mass and obesity-associated (FTO) protein contributes to non-syndromic human obesity which refers to excessive fat accumulation in human body and results in health risk. FTO protein has become a promising target for anti-obesity medicines as there is an immense need for the rational design of potent inhibitors to treat obesity. In our study, a new scaffold N-phenyl-1H-indol-2-amine was selected as a base for FTO protein inhibitors...
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Design, synthesis, and molecular docking of new 5-HT reuptake inhibitors based on modified 1,2-dihydrocyclopenta[b] indol-3(4H)-one scaffold
PublicationA new group of serotonin reuptake inhibitors containing 1,2-dihydrocyclopenta[b]indol-3(4H)-one scaffoldwas synthesized, starting from indole 5-((1H-indol-3-yl)(1,3-dioxane-4,6-diones as a key intermediates. Following three transformations including intramolecular cyclization and formation of imines, a series of new ligand for human serotonin transporter was obtained. The ability of these ligands to inhibit human TS3 serotonin transporter...
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Optimization of Chemical Functionalities of Indole-2-carboxamides To Improve Allosteric Parameters for the Cannabinoid Receptor 1 (CB1)
Publication5-Chloro-3-ethyl-N-(4-(piperidin-1-yl)phenethyl)-1H-indole-2-carboxamide (1; ORG27569) is a prototypical allosteric modulator for the cannabinoid type 1 receptor (CB1). Here, we reveal key structural requirements of indole-2-carboxamides for allosteric modulation of CB1: a critical chain length at the C3-position, an electron withdrawing group at the C5-position, the length of the linker between the amide bond and the phenyl ring...
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Impact of blocking layer on DSSC performance based on new dye -indolo[3,2,1-jk]carbazole derivative and N719
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New thiourea organocatalysts and their application for the synthesis of 5-(1H-indol-3-yl)methyl-2,2-dimethyl-1,3-dioxane-4,6-diones a source of chiral 3-indoylmethyl ketenes
PublicationThe stereoselective properties of modified thiourea organocatalysts were tested in the Friedel–Crafts alkylation of indole with 5-arylidene-2,2-dimethyl-1,3-dioxane-4,6-diones, which produces chiral 5-((1H-indol-3-yl)(aryl)methyl)-2,2-dimethyl-1,3-dioxane-4,6-diones. Based on a tentative reaction mechanism for ((S)-N-benzyl-2-(3-(3,5-bis (trifluoromethyl)phenyl)thioureido)-N,3,3-trimethylbutanamide organocatalysts, modifications...
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Indo American Journal of Pharmaceutical Sciences
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Ultrasound assisted rapid synthesis of mefenamic acid based indole derivatives under ligand free Cu-catalysis: Their pharmacological evaluation
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Amberlyst-15 catalysed synthesis of novel indole derivatives under ultrasound irradiation: Their evaluation as serotonin 5‑HT2C receptor agonists
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Modulation of rat hepatic and kidney phase II enzymes by cabbage juices: comparison with the effects of indole-3-carbinol and phenethyl isothiocyanate
PublicationZbadano wpływ soków ze świeżej i kiszonej kapusty na ekspresję i aktywność takich enzymów II fazy jak transferazy S-glutationowe i oksydoreduktaza NQO1 w wątrobie i nerkach szczurów, którym podawano wspomniane soki doustnie. Uzyskane wyniki porównano z oznaczeniami uzyskanymi po doustnym podaniu wyizolowanych produktów degradacji glukozynolanów, indolo-3-karbinolu i izotiocyjanianu fenyloetylu. Wszystkie testowane czynniki powodowały...
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Amberlyst-15 catalysed synthesis of novel indole derivatives under ultrasound irradiation: Their evaluation as serotonin 5‑HT2C receptor agonists
PublicationA series of indole based novel Schiff bases was designed as potential agonists of 5‑HT2C receptor that was supported by docking studies in silico. These compounds were synthesized via Amberlyst-15 catalysed condensation of an appropriate pyrazole based primary amine with the corresponding indole-3-aldehyde under ultrasound irradiation at ambient temperature. A number of target Schiff bases were obtained...
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Modulation of CYP19 expression by cabbage juices and their active components: indole-3-carbinol and 3,30-diindolylmethene in human breast epithelial cell lines
PublicationThe aim of this study was to evaluate the effect of white cabbage and sauerkraut juices of different origin and indole-3-carbinol (I3C) and diindolylmethane (DIM) on expression of CYP19 gene encoding aromatase, the key enzyme of estrogen synthesis.Remarkable differences in the effect on CYP19 transcript and protein level were found between the cab- bage juices (in 2.5-25 mL/L concentrations) and indoles (in 2.5-50 lM doses) in...
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Modulation of carcinogen metabolizing cytochromes p450 in rat liver and kidney by cabbage and sauerkraut juices: comparison with the effects of indole-3-carbinol and phenethyl isothiocyanate
PublicationThis study investigated the effect of raw cabbage and sauerkraut juices on the activity and expression of CYP1A1, 1A2, 1B1 and 2B in Wistar rat liver and kidney. The results were compared with those of two commercially available products of glucosinolates degradation: indole-3-carbinol (I3C) and phenethyl isothiocyanate (PEITC). Significant differences in the effect of the cabbage juices as well as I3C and PEITC between the liver...
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Propargylamines in Pd/Cu-catalyzed tandem coupling-cyclization-N-deprotection in a single pot: Construction of N-unsubstituted vs N-sulfonyl indole ring
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The Strategic Partnership Between India and the United States of America and How China’s Influence Challenges the India-Us Alliance in the Indo-Pacific Region
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IPPA bulletin (Bulletin of the Indo-Pacific Prehistory Association)
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Novel isatin–indole derivatives as potential inhibitors of chorismate mutase (CM): their synthesis along with unexpected formation of 2-indolylmethylamino benzoate ester under Pd–Cu catalysis
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Opracowanie nowych metodyk oznaczeń ilościowych i jakościowych izotiocyjanianów oraz związków indolowych w próbkach roślin z rodziny Brassicaceae
PublicationIzotiocyjaniany (ITC) i indole powstające w wyniku hydrolizy glukozynolanów obecnych w roślinach z rodziny Brassicaceae wykazują wysoką aktywność biobójczą w stosunku do fitofagów stanowiąc alternatywę dla syntetycznych pestycydów. Zaliczane są także do najważniejszych żywieniowych substancji przeciwzapalnych i przeciwrakotwórczych. Pomimo wielu zastosowań dotychczas brakowało metod analitycznych umożliwiających ich rutynowe oznaczanie....
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Andrzej Okuniewski dr inż.
PeopleEducation 2010-2014: Department of Inorganic Chemistry, Faculty of Chemistry, Gdańsk University of TechnologyPhD in chemical sciences (chemical sciences - chemistry, inorganic chemistry) 2009-2010: Faculty of Chemistry, Gdańsk University of TechnologyMaster of Chemistry (applied chemistry) 2005-2009: Faculty of Chemistry, Gdańsk University of Technologychemical engineer (applied chemistry) 2002-2005: II High School Władysław Pniewski...
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Effect of culinary treatment on chnages in the contents of selected nutrients and non-nutrients in curly kale (Brassica oleracea var. acephala)
PublicationKale has a great nutritive value, very high antioxidant activity and pro-healthypotential. The level of phytochemicals and related bioactive compounds arestrongly dependent on pre and postharvest stages of production chain (domestic orindustrial). The study investigated changes in the levels of vitamin C, b-carotene,total polyphenols, antioxidant activity, degradation products of glucosinolates aswell as nitrates and nitrites in...
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Improved degradation of etodolac in the presence of core-shell ZnFe2O4/SiO2/TiO2 magnetic photocatalyst
PublicationIn the present study, susceptibility to photocatalytic degradation of etodolac, 1,8-diethyl-1,3,4,9 – tetrahydro pyran - [3,4-b] indole-1-acetic acid, which is a non-steroidal anti-inflammatory drug frequently detected in an aqueous environment, was for the first time investigated. The obtained p-type TiO2-based photocatalyst coupled with zinc ferrite nanoparticles in a core-shell structure improves the separation and recovery...
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Covalent DNA modification by products of myrosinase catalysed glucosinolate degradation in cell-free system
PublicationThe bioactive phytochemicals found in Brassica vegetables belonging to glucosinolates (GLS) and especially the products of their degradation isothiocyanates (ITC) and indoles are regarded as the most promising cancer chemopreventive compounds. These secondary metabolites constitute defence system repelling or preventing the development of agrophages attacking brassica plants. The antibiological properties of these compounds suggest...
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Simultaneous Determination of Indolic Compounds in Plant Extracts by Solid-Phase Extraction and High-Performance Liquid Chromatography with UV and Fluorescence Detection
PublicationA high-performance liquid chromatographic method with UV and fluorescence detection (HPLC-DAD-FLD) was developed for simultaneous determination of indolic compounds in plant material. Indole-3-carbinol (I3C), indole-3-acetic acid (I3AA), indole-3-acetonitrile (I3ACN), and 3,3′-diindolylmethane (DIM) were used as representative compounds that cover a wide spectrum of indole structures occurring in nature. For concentration and purification...
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Transition-Metal-Promoted Oxidative Cyclization To Give 1,2,4-Trisubstituted Carbazole Scaffolds
PublicationHerein, we describe the synthesis of a 1,2,4-trisubstituted carbazole core from 5-(1H-indol-3-yl)-3-oxopentanoic acid esters or amides. For oxidative cyclization, we tested two different approaches. First, we used manganese triacetate as a conventional moderate oxidizer to ensure the radical course of the reaction. Second, we examined the use of a more complex oxidizing agent I2/Me(OTf)3. In both cases, formation of a fused-ring...
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Inhibitory mikrotubul w terapii przeciwnowotworowej = Inhibitors of microtubule in cancer therapy
PublicationW artykule opisano inhibitory mikrotubul, różnorodne związki chemiczne, znajdujące się w zaawansowanych przedklinicznych i wstępnych badaniach klinicznych. Pośród nich na uwagę zasługują półsyntetyczne analogi taksolu, substancje pochodzenia naturalnego, takie jak: epotilony, kombretastatyny, kolchinoidy, dolastatyny oraz syntetyczne związki o niskim ciężarze czasteczkowym: heterokombretastatyny, sulfonamidy, fenostatyny, pochodne...
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Identification of 1H‐indene‐(1, 3, 5, 6)‐tetrol derivatives as potent pancreatic lipase inhibitors using molecular docking and molecular dynamics approach
PublicationPancreatic lipase is a potential therapeutic target to treat diet-induced obesity in humans, as obesity-related diseases continue to be a global problem. Despite intensive research on finding potential inhibitors, very few compounds have been introduced to clinical studies. In this work, new chemical scaffold 1H-indene-(1,3,5,6)-tetrol was proposed using knowledge-based approach, and 36 inhibitors were derived by modifying its...
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Effect of cooking on the contents of glucosinolates and their degradation products in selected Brassica vegetables
PublicationChanges in the levels of glucosinolates and their degradation products in selected Brassica vegetables due to the cooking process were investigated. The purple cauliflower was found to be the best source of aliphatic and indole glucosinolates, and it was also abundant in compounds such as sinigrin, glucoraphanin and glucobrassicin. As a result of cooking rutabaga, green cauliflower and purple cauliflower, a significant decrease...
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Effect of conventional cooking on changes in the contents of basic composition and glucosinolates in kale
PublicationBrassica vegetables have been strongly recommended as part of human diet because of its high content of bioactive sulphur compounds, eg glucosinolates. The nutrient and health promoting compounds in kale are significantly affected by traditional cooking. The study investigated changes in the levels of dry mass, ash, fat, total protein, dietary fibre as well as total and individual glucosinolates in the kale due to the traditional...
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From tryptophan to novel mitochondria-disruptive agent, synthesis and biological evaluation of 1,2,3,6-tetrasubstituted carbazoles
PublicationMitochondrial targeting plays an important role in anticancer therapy. The Mn(III)-promoted cyclization of 5- (1H-indol-3-yl)-3-oxopentanoic acid allow to obtain novel substituted carbazole derivatives that can act as mitochondria-disruptive agents. The starting materials used for the synthesis of these new aminocarbazoles are oxopentanoate derivatives of tryptophan. The scope and limitation of this method of synthesis are determined...
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Molecular differences in mitochondrial DNA (mtDNA) genomes of dogs with malignant mammary tumours
Open Research DataThe aim of this study was to determine molecular defects in mitochondrial DNA with the use of large-scale genome analysis in malignant canine mammary gland tumours and indicate whether these changes were linked with the carcinogenesis process. With the use of the NGS technology, we sequenced 27 samples of mtDNA isolated from blood and tumours obtained...
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Glukozynolany: znaczenie i metody oznaczania
PublicationWarzywa krzyżowe wzbudzają zainteresowanie badaczy jako potencjalne źródło substancji mogących znaleźć zastosowanie w profilaktyce chorób nowotworowych. Przeciwrakotwórcze właściwości tych roślin wiązane są z obecnością glukozynolanów i produktów ich rozkładu, tj. izotiocyjanianów i indoli, które wykazują wiele aktywności biologicznych istotnych z punktu widzenia chemoprewencji nowotworów. Wspomniane związki mają również aktywność...
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Modulation of CYP1A1, CYP1A2 and CYP1B1 expression by cabbage juices and indoles in human breast cell lines
PublicationEpidemiological studies have shown that consumption of cab- bage and sauerkraut is connected with significant reduction of breast cancer incidences. Estrogens are considered a major breast cancer risk factor and their metabolism by P450 enzymes substan- tially contributes to carcinogenic activity. The aim of this study was to investigate the effect of cabbage and sauerkraut juices of differ- ent origin on the expression profile...
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Opracowanie dogodnej metody tworzenia wiązań S-C o hybrydyzacji atomu węgla sp oraz sp2
PublicationBadania przeprowadzone w Katedrze Chemii Organicznej Wydziału Chemicznego Politechniki Gdańskiej na przestrzeni ostatnich kilku lat, pokazały wszechstronność pochodnych kwasu neopentylidenofosforoditiowego. Dotychczasowe wyniki badań doprowadziły mnie do opracowania nowych strategii syntetycznych, umożliwiających otrzymywanie związków zawierających wiązanie C-S o hybrydyzacji atomu węgla sp oraz sp2. Analizując wyniki badań opracowałam...
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The comparison of cytotoxic and genotoxic activities of glucosinolates, isothiocyanates, and indoles
PublicationChemopreventive properties of Brassica vegetables are attributed mainly to their characteristic compounds—glucosinolates (GLs) and their main hydrolysis products—isothiocyanates (ITCs) and indoles. In this study, we compared antiproliferative activity (MTT test in HT29 cells) and genotoxic effects (comet assay in HT29 cells and restriction analysis in a cell-free system) of three GLs (sinigrin (SIN), glucotropaeolin (GTL), and...
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Encapsulation of an anticancer drug Isatin inside a host nano-vehicle SWCNT: a molecular dynamics simulation
PublicationThe use of carbon nanotubes as anticancer drug delivery cargo systems is a promising modality as they are able to perforate cellular membranes and transport the carried therapeutic molecules into the cellular components. Our work describes the encapsulation process of a common anticancer drug, Isatin (1H-indole-2,3-dione) as a guest molecule, in a capped single-walled carbon nanotube (SWCNT) host with chirality of (10,10). The...