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Steroid sulfatase inhibitors based on sulfamated derivatives of 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenol as potential anticancer agents
ProjectsProject realized in Department of Inorganic Chemistry according to TANGO-IV-A/0004/2019-00 agreement from 2020-08-28
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Andrzej Miszczyk dr hab. inż.
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L-Homoserine O-acetyltransferase (CaMet2p) activity and inhibition
Open Research DataThe 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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Evaluation of antimicrobial properties of thermomelt adhesives modified with zinc compounds
Open Research DataThe dataset contains the results of microbiological tests of thermomelt adhesives modified with zinc compounds, whose activity was assessed for their ability to reduce the number of Escherichia coli and Staphylococcus aureus strain, representing the Gram (-) and Gram (+) bacteria, respectively. The evaluation of antimicrobial properties of samples were...
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Synthesis and biological activity of novel ester derivatives of N3-(4-metoxyfumaroyl)-(S)-2,3-diaminopropanoic acid containing amide and keto function as inhibitors of glucosamine-6-phosphate synthase
PublicationA short series of novel ester derivatives of N3-4-methoxyfumaroyl-(S)-2,3-diaminopropanoic acid (FMDP) containing amido or keto functions have been designed and synthesized. Their antifungal activity and inhibitory properties toward fungal glucosamine-6-phosphate synthase has also been evaluated. The obtained compounds 11-13 and 15-17 demonstrated good antifunga activity against Candida albicans. Compounds 11-13 displayed also...
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Synthesis and biological evaluation of fluorinated 3-phenylcoumarin-7-O-sulfamate derivatives as steroid sulfatase inhibitors
PublicationIn 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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New potent STS inhibitors based on fluorinated 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamates
PublicationA series of fluorinated analogs based on the frameworks of 4-(1- phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamates have been synthesized as steroid sulfatase (STS) inhibitors. The design of chemical structures of new potential STS inhibitors was supported by molecular docking techniques to identify potential interactions between inhibitors and amino acid residues located in the STS active site. The STS inhibitory potency was evaluated...
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Antifungal Activity of Homoaconitate and Homoisocitrate Analogs
PublicationThirteen structural analogs of two initial intermediates of the L-alpha-aminoadipate pathway of L-lysine biosynthesis in fungi have been designed and synthesized, including fluoro- and epoxy-derivatives of homoaconitate and homoisocitrate. Some of the obtainedcompounds exhibited at milimolar range moderate enzyme inhibitory properties against homoaconitase and/or homoisocitrate dehydrogenase of Candida albicans. The structural...
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Recent progress in the development of steroid sulfatase inhibitors – examples of the novel and most promising compounds from the last decade
PublicationThe purpose of this review article is to provide an overview of recent achievements in the synthesis of novel steroid sulfatase (STS) inhibitors. STS is a crucial enzyme in the biosynthesis of active hormones (including estrogens and androgens) and, therefore, represents an extremely attractive molecular target for the development of hormone-dependent cancer therapies. The inhibition of STS may effectively reduce the availability...
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Solubilization of keratins and functional properties of their isolates and hydrolysates
PublicationThe keratinous wastes of the textile industry and poultry slaughterhouses may be used as sources of soluble keratins or hydrolysates. This review presents methods for processing raw keratin-based materials into bioproducts with functional and bioactive properties suitable for biomedical, cosmetic, food, and agricultural applications. Soluble keratin can be obtained by thermal treatment in some organic solvents, reduction, or oxidation...
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Synthesis and biological evaluation of N-acylated tyramine sulfamates containing C-F bonds as steroid sulfatase inhibitors
PublicationSteroid 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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Design, synthesis and biological evaluation of novel N-phosphorylated and O-phosphorylated tacrine derivatives as potential drugs against Alzheimer’s disease
PublicationIn this work, we designed, synthesised and biologically investigated a novel series of 14N- and O-phosphorylated tacrine derivatives as potential anti-Alzheimer’s disease agents. In the reaction of 9-chlorotacrine and corresponding diamines/aminoalkylalcohol we obtained diamino and aminoalkylhydroxy tacrine derivatives. Next, the compounds were acid to give final products 6–13 and 16–21 that were characterised by 1H, 13 C, 31P...
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Synthesis, anticandidal activity of N3-(4-methoxyfumaroyl)-(S)-2,3-diaminopropanoic amide derivatives – Novel inhibitors of glucosamine-6-phosphate synthase
PublicationNovel FMDP amiders 4-6 have been synthesized and tested against Candida strains. The anticandidal activity has been confined only to Candida albicans. Anticandidal activity of the tested amides has correlated with their inhibitory activity of glucosamine-6-phosphate synthase in cell free extract from Candida albicans.
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Pretreatment of Lignocellulosic Materials as Substrates for Fermentation Processes
PublicationLignocellulosic biomass is an abundant and renewable resource that potentially contains large amounts of energy. It is an interesting alternative for fossil fuels, allowing the production of biofuels and other organic compounds. In this paper, a review devoted to the processing of lignocellulosic materials as substrates for fermentation processes is presented. The review focuses on physical, chemical, physicochemical, enzymatic,...
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Synthesis of bicoumarin thiophosphate derivatives as steroid sulfatase inhibitors
PublicationBased on the frameworks 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, a series of bicoumarin thiophosphate analogs have been synthesized and biologically evaluated. Additionally, their binding modes have been modeled using docking techniques. The inhibitory properties of the synthesized compounds...
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Transport deficiency is the molecular basis of Candida albicans resistance to antifungal oligopeptides
Publication(FMDP), an inhibitor of glucosamine-6-phosphate synthase, exhibited growth inhibitory activity against Candida albicans, with minimal inhibitory concentration values in the 0.05–50 mg/L range. Uptake by the peptide permeases was found to be the main factor limiting an anticandidal activity of these compounds. Di- and tripeptide containing FMDP (F2 and F3) were transported by Ptr2p/Ptr22p peptide transporters (PTR) and FMDP-containing...
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Novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(1,3,5-triazin-2-ylamino)guanidine derivatives: Inhibition of human carbonic anhydrase cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII, anticancer activity, and molecular modeling studies
PublicationA series of novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(6-substituted-4-chloro-1,3,5-triazin-2-ylamino)guanidine derivatives 9–20 have been synthesized by substitution of chlorine atom at the 1,3,5-triazine ring in compounds 5–8 with 3- or 4-aminobenzenesulfonamide and 4-(aminomethyl)benzenesulfonamide hydrochloride. All the synthesized compounds were evaluated for their inhibitory activity toward hCA I, II,...
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Chemical and biological characterization of Ocimum basilicum L. phenolic extract and essential oil derived through ultrasound and microwave-assisted extraction techniques
PublicationPlant-derived bioactive molecules are increasingly utilized in food processing as natural additives, driven by a growing interest in healthier lifestyles. This trend has spurred industries to reformulate products to meet the demands of health-conscious consumers. This study investigates the phenolic extract and essential oil of O. basilicum L. obtained via ultrasound-assisted extraction and microwave-assisted extraction, respectively. Characterization...
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Chitosan and polyvinyl alcohol nanocomposites with cellulose nanofibers from ginger rhizomes and its antimicrobial activities
PublicationThe inhibitory effect of 5% GNF bionanocomposites against Bacillus cereus, Escherichia coli, Staphylococcus aureus and Salmonella typhimurium indicated good antibacterial activity of the nanocomposites due to the addition of GNF in the biopolymer matrices. The use of GNF will help to increase the economic values of agricultural waste and the characteristic properties of GNF derived bionanocomposites could be possibly used in medical...
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Steroid Sulfatase Inhibitors Based on Phosphate and Thiophosphate Flavone Analogs
PublicationA series of phosphate and thiophosphate flavone derivatives were synthesized and biologically evaluated in vitro for inhibition of steroid sulfatase (STS) activity. The described synthesis includes the straightforward preparation of 7-hydroxy-2-phenyl-4H-chromen-4-one 3a, 2-(4-fluorophenyl)-7-hydroxy-4H-chromen-4-one 3b, 7-hydroxy-2-(4-(trifluoromethyl)phenyl)-4H-chromen-4-one 3c, 7-hydroxy-2-(p-tolyl)-4H-chromen-4-one 3d modified...
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N-Alkyl Derivatives of L-Glutamine As Inhibitors of Glutamine - Utilizing Enzymes
PublicationA general facile method to synthesize the N-gamma-alkyl and N-gamma,N-gamma-dialkyl derivatives of L-glutamine (1a-d) from L-glutamic acid as a starting substrate is presented. The obtained compounds are shown to inhibit three diferent glutamine-utilizing enzymes, namely: glutaminase, gamma-glutamyl transpeptidase, and glucosamine-6-phosphate synthase, with inhibitory constants within the milimolar range.
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N-acylpeptides with glucosamine-6-phosphate synthase inhibitors - synthesisand antifungal activity
PublicationOpracowano syntezę kilku peptydów (di i tripeptydów) zawierających inhibitory syntazy glukozamino-6-fosforanu oraz przeprowadzono je w N-acylopochodne (acetylowe, heksanoilowe, dekanoilowe) oraz zbadano ich aktywność przeciwgrzybową w stosunku do szczepów Candida albicans z opornością wielolekową. Stwierdzono, że N-acylopeptydy wykazują aktywność przeciwgrzybową oraz określono wartości MIC.
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Effect of antitumor compounds on the yeast topoisomerase II relaxation activity
Open Research DataThe datasets contain results of antitumor compounds* (known inhibitors of human topoisomerase alpha II) inhibitory activity against yeast topoisomerase II. DNA topoisomerases (Topo) are enzymes that catalyze changes in the spatial structure of DNA and play an important role in replication, transcription and recombination. Beyond their normal functions,...
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Synergistic Effects of Propolis Combined with 2-Phenoxyethanol and Antipyretics on the Growth of Staphylococcus aureus
PublicationThe present investigation aimed to assess the combinational effect of commonly usedantipyretics and antiseptics with ethanolic extracts of propolis (EEPs) on the growth inhibition ofStaphylococcus aureus. The broth microdilution checkerboard assay revealed synergistic interactionsbetween all investigated antipyretics, namely acetylsalicylic acid, ibuprofen, and acetaminophen,with EEPs samples. The values of the fractional inhibitory...
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Projektowanie, synteza fosforowych i tiofosforowych pochodnych kumaryny, bifenylu, tyraminy oraz flawonoidów i badanie ich aktywności biologicznej jako potencjalnych inhibitorów sulfatazy steroidowej (STS)
PublicationChoroby nowotworowe są jednym z najpoważniejszych problemów z jakimi zmaga się współczesne społeczeństwo. Rak piersi jest jedną z głównych przyczyn zgonów wśród kobiet w krajach rozwiniętych, dlatego też niezbędne jest opracowanie nowych, skutecznych metod leczenia. Podstawowym problemem w selektywnym zwalczaniu komórek nowotworowych jest ich wysokie podobieństwo do komórek prawidłowych. W związku z dowodami na znaczący udział...
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Glucosinolates from lepidium peruvianum as potential antiamnestic drugs
PublicationLepidium peruvianum (maca) (Brassicaceae) is a naturally occurring plant mainly in the high Andes of Peru. In recent years, it has been intensively researched in terms of its influence on various diseases and towards health improvement. Alzheimer’s disease is an incurable disease that most often affects adults over the age of 60. As since 2003 the US Food and Drug Administration (FDA) did not approve any new drug for Alzheimer’s...
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Implication of the disulfide bridge in trypsin inhibitor SFTI-1 in its interaction with serine proteinases
PublicationFourteen monocyclic analogues of trypsin inhibitor SFTI-1 isolated from sunflower seeds were synthesized by the solid-phase method. The purpose of this work was to establish the role of a disulfide bridge present in inhibitor's side chains of Cys3 and Cys11 in association with serine proteinases. This cyclic fragment was replaced by the disulfide bridges formed by L-pencillamine (Pen), homo-L-cysteine (Hcy), N-sulfanylethylglycine...
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Fatty acyl benzamido antibacterials based on inhibition of DnaK-catalyzed protein folding
PublicationWe have reported that the hsp70 chaperone DnaK from Escherichia coli might assist protein folding by catalyzing the cis/trans isomerization of secondary amide peptide bonds in unfolded or partially folded proteins. In this study a series of fatty acylated benzamido inhibitors of the cis/trans isomerase activity of DnaK was developed and tested for antibacterial effects in E. coli MC4100 cells. Nα-[Tetradecanoyl-(4-aminomethylbenzoyl)]-l-asparagine...
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The impact of equity pledge on inefficient investment: a perspective from family entrepreneurship
PublicationAs an efficient and convenient financing method, equity pledges may have a heterogeneous impact on the inefficient investment of family firms. In order to verify this point, this paper takes A-share listed family enterprises from 2010 to 2021 as a research sample. It conducts an empirical test on the impact of equity pledges on inefficient investment in family firms by constructing a panel regression model. The results show...
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Kinetic characterization of hydrogen sulfide inhibition of suspended anammox biomass from a membrane bioreactor
PublicationThe inhibition effects of hydrogen sulfide (H2S) on anammox-enriched biomass from a laboratory membrane reactor were analyzed in a series of batch respirometric experiments. The determined half maximal inhibitory concentration (IC50) was 4.67 mg H2S-S L−1 at the constant pH = 7.0 and the total sulfide concentration varying between 1 and 15 mg TS-S L−1. In another test, the IC50 was found to be 4.25 mg H2S-S L−1 under a constant...
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Phosphate tricyclic coumarin analogs as steroid sulfatase inhibitors: synthesis and biological activity.
PublicationIn 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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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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Fatty acids as molecular carriers in cleavable antifungal conjugates
PublicationConjugates composed of C2-18 fatty acid (FA) residues as a molecular carrier and 5-fluorocytosine (5-FC) as an active agent, released upon the action of intracellular esterases on the ester bond between FA and “trimethyl lock” intramolecular linker, demonstrate good in vitro activity against human pathogenic yeasts of Candida spp. The minimal inhibitory concentrations (MIC) values for the most active conjugates containing caprylic...
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Antifungal Activity of Capridine β as a Consequence of Its Biotransformation into Metabolite Affecting Yeast Topoisomerase II Activity
PublicationIn 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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Divulging the anti-acetylcholinesterase activity of Colletotrichum lentis strain KU1 extract as sustainable AChE active site inhibitors
PublicationAlzheimer’s disease (AD), also called senile dementia is a neurodegenerative disease seen commonly in the elderly and is characterised by the formation of β-amyloid plaques and neurofbrillary tangles (NFT). Though a complete understanding of the disease is lacking, recent studies showed the role of the enzyme acetylcholinesterase (AChE) in pathogenesis. Finding new lead compounds from natural sources has always been a quest for...
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Taq DNA polymerase fused with DNA binding protein with increased resistance to inhibitors from clinical samples
PublicationNowadays PCR method is commonly used in molecular diagnostic. However, in many cases PCR is limited, by the presence of inhibitory substances in biological, soil or food samples Efficiency and fidelity of amplification is strongly connected with DNA polymerase and reaction conditions. To meet the requirements of modern diagnostic methods it is essential to seeking for new DNA polymerases with better properties useful in these field....
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Bee Bread Exhibits Higher Antimicrobial Potential Compared to Bee Pollen
PublicationThis study aimed at investigation of the antimicrobial potential of ethanolic extracts of bee bread (BB) and bee pollen (BP) and suspensions of these products in MHB (Mueller Hinton Broth). We covered 30 samples of BP and 19 samples of BB harvested in Polish apiaries. Slightly lower activity was observed against Gram-negative bacteria compared to Gram-positive staphylococci. BB extracts exhibited higher inhibitory potential with...
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The impact of training and neurotrophins on functional recovery after spinal cord transection: cellular and molecular mechanisms contributing to motor improvement
PublicationBeneficial effects of locomotor training on the functional recovery after complete transection of the spinal cord indicate that in chronic spinal animals spontaneous recovery processes are enhanced and shaped by the training. The mechanisms of that use-dependent improvement are still not fully understood. This review tackles three aspects of this issue: (1) neurochemical attributes of functional improvement...
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Synthesis and biological evaluation of fluorinated N-benzoyl and N-phenylacetoyl derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as steroid sulfatase inhibitors
PublicationIn the present work, we report convenient methods for the synthesis of 3-(4-aminophenyl)-coumarin-7-O-sulfamate derivatives N-acylated with fluorinated analogues of benzoic or phenylacetic acid as steroid sulfatase (STS) inhibitors. The design of these potential STS inhibitors was supported by molecular modeling techniques. Additionally, computational docking methods were used to determine the binding modes of the synthesized inhibitors...
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Catalytic topoisomerase II inhibitors in cancer therapy.
PublicationDNA topoizomeraza II jest jednym z głównych celów molekularnych dla leków stosowanych w terapii przeciwnowotworowej. Wszystkie inhibitory tego enzymu są zdolne do zakłócania w jeden z etapów cyklu katalitycznego topoizomerazy II. Związki, które stabilizują kowalencyjny kompleks DNa i topoizomerazy II (znany jako kompleks rozszczepialny) są nazywane truciznami topoizomerazy, inne związki, które hamują aktywność enzymu na innych...
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Multidirectional Characterization of Phytochemical Profile and Health-Promoting Effects of Ziziphora bungeana Juz. Extracts
PublicationZiziphora species (Lamiaceae) have been used in traditional medicine as sedatives, anti-septics, carminatives, or expectorants. Despite their common applications in phytotherapy, there is still lack of evidence about the composition of their extracts and its impact on biological properties of the plants. The aim of this study was to evaluate the content of Ziziphora bungeana, a less studied species growing in Kazakhstan, using...
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Phosphate and Thiophosphate Biphenyl Analogs as Steroid Sulfatase Inhibitors
PublicationIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate and thiophosphate biphenyl derivatives exhibiting steroid sulfatase (STS) activity. The described synthesis is based on straightforward preparation of biphenyl-4-ol and 40-hydroxybiphenyl- 4-carboxylic acid ethyl ester modified with various phosphate or thiophosphate moieties. The inhibitory effects of these compounds were...
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The inhibition effect of mad Honey on corrosion of 2007-type aluminium alloy in 3.5% NaCl solution
PublicationThe inhibition effect of mad honey on corrosion of 2007-type aluminium alloy in 3.5% NaCl solution was investigated by Tafel extrapolarisation (TP), electrochemical impedance spectroscopy (EIS) and dynamic electrochemical impedance spectroscopy (DEIS). All the studied parameters exhibited good anti-corrosive properties against corrosion of 2007-type aluminium alloy in the test solution; the corrosion rates decreased with the increase...
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Synthesis of analogues of anthraquinones linked to tuftsin or retro-tuftsin residues as potential topoisomerase inhibitors
PublicationZsyntetyzowano 10 nowych analogów antrachinonów z pochodnymi tuftsyny i retro-tuftsyny jako potencjalne inhibitory topoizomerazy. Substratem wyjściowym były zsyntetyzowane 1,4-, 1,5- i 1,8-bis(tosyloksy)-9,10-antrachinony oraz odpowiednio chronione pochodne tuftsyny i retro-tuftsyny, które otrzymano metodą mieszanych bezwodników z zastosowaniem chloromrówczanu izobutylu i NMM. Reakcje prowadzone były w acetonitrylu pod azotem w...
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Białka aktywne biologicznie obecne w soku pokrochmalnianym
PublicationPodczas przetwarzania 1 tony ziemniaków na skrobię powstaje od 5 do 12 m3 odpadów ciekłych, które zawierają 300-410 g białek na 1 kg suchej masy. Trzy główne grupy białek to: białka typu patatyny, inhibitory proteaz o charakterze zasadowym, grupa białek złożonych o wielkości 22 kDa. Białka te mogą zostać wyizolowane z soku pokrochmalnianego w formie natywnej, a następnie wykorzystane jako: środki ochrony roślin, dodatki do żywności...
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The Distribution of Glucosinolates in Different Phenotypes of Lepidium peruvianum and Their Role as Acetyl- and Butyrylcholinesterase Inhibitors—In Silico and In Vitro Studies
PublicationThe aim of the study was to present the fingerprint of different Lepidium peruvianum tu- ber extracts showing glucosinolates-containing substances possibly playing an important role in preventinting dementia and other memory disorders. Different phenotypes of Lepidium peruvianum (Brassicaceae) tubers were analysed for their glucosinolate profile using a liquid chromatograph coupled with mass spectrometer (HPLC-ESI-QTOF-MS/MS platform)....
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Novel steroid sulfatase inhibitors based on N ‐thiophosphorylated 3‐(4‐aminophenyl)‐coumarin‐7‐O‐sulfamates
PublicationIn the present work, we described convenient methods for the synthesis ofN-thiophosphorylated 3-(4-aminophenyl)-coumarin-7-O-sulfamates as steroid sulfatase(STS) inhibitors. To design the structures of the potential STS inhibitors, molecularmodeling techniques were used. A computational docking method was used to deter-mine the binding modes of the synthesized inhibitors as well as to identify potentialinteractions between specified...
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Emerging anticancer activity of candidal glucoseamine-6-phosphate synthase inhibitors upon nanoparticle-mediated delivery
PublicationNumerous 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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Drug-drug interaction potential of antitumor acridine agent C-1748: The substrate of UDP-glucuronosyltransferases 2B7, 2B17 and the inhibitor of 1A9 and 2B7
PublicationBackground The compound 9-(2′-hydroxyethylamino)-4-methyl-1-nitroacridine (C-1748), the promising antitumor agent developed in our laboratory was determined to undergo phase I metabolic pathways. The present studies aimed to know its biotransformation with phase II enzymes – UDP-glucuronosyltransferases (UGTs) and its potential to be engaged in drug-drug interactions arising from the modulation of UGT activity. Methods UGT-mediated...
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Selected symmetrically substituted carbazoles: Investigation of anticancer activity and mechanisms of action at the cellular and molecular levels
PublicationDNA topoisomerases play a critical role as essential enzymes in controlling alterations in the topology of DNA. They achieve this by orchestrating the coordinated process of breaking and rejoining DNA strands, which is crucial for maintaining the proper structure of DNA during regular cellular development. The search for and development of new potential anticancer drugs is a challenging yet immensely important area of research...