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Search results for: SELECTIVE LIGANDS
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3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands
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Chromogenic derivatives of new bis(phenylhydrazono-1H-tetrazol-5-yl-acetonitriles) - synthesis and properties
PublicationDerivatives of bis(phenylhydrazono-1H-tetrazol-5-yl-acetonitriles) with oxygen and sulphur atoms in the structure of aliphatic chains were successfully synthesised. The correlation between the ligand structure and its complexation properties was investigated by absorption spectroscopy. The formation of complexes of presented compounds with metal cations (Cu2+, Ni2+, Zn2+, Co2+, Fe2+ and Pb2+) was studied. Ligands 5-8 were additionally...
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Cancer-selective, single agent chemoradiosensitising gold nanoparticles
PublicationTwo nanometre gold nanoparticles (AuNPs), bearing sugar moieties and/or thiol-polyethylene glycol-amine (PEG-amine), were synthesised and evaluated for their in vitro toxicity and ability to radiosensitise cells with 220 kV and 6 MV X-rays, using four cell lines representing normal and cancerous skin and breast tissues. Acute 3 h exposure of cells to AuNPs, bearing PEG-amine only or a 50:50 ratio of alpha-galactose derivative and...
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New clicked full agonists of the estrogen receptor β
PublicationA click chemistry approach was used to synthesize a series of 1,4-diaryl-substituted 1,2,3-triazoles designed to behave as estrogen receptor (ER) ligands. We studied their affinities for both receptors α and β, their agonist activities in a cell-based luciferase reporter assay and their effect on the proliferation of the hormone-dependent MCF-7 cell line. We found two compounds (3a and 3c) that behave as selective full agonists...
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Lower rim substituted p-tert-butyl-calix[4]arene. Part 17. synthesis, extractive and ionophoric properties of p-tert-butylcalix[4]arene appended with hydroxamix acid moieties
PublicationThe synthesis and characterization of four p-tert-butylcalix[4]arene-hydroxamic acidc are reported. The dependence of the metal ion binding, assessed by liquid extraction of the metal nitrates from water into dichloromethane in individual and competitive experiments, on the ligand structure, is presented. The results showed that those ligands could be successfully used in separation process of trnasition and heavy metals often...
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Gold nanoparticles and their coatings, their effect on cells and their interaction with radiation
PublicationTwo nanometre gold nanoparticles (AuNPs), bearing sugar moieties and/or polyethylene glycolamine (PEG-amine), were synthesised and evaluated for their in vitro toxicity and ability to radiosensitise cells with 220 kV and 6 MV X-rays, using four cell lines representing normal and cancerous skin and breast tissues. In addition to the observed intrinsic cancer-selective chemotoxicity, these AuNPs acted as radiosensitisers in combination with...
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Calix[4]arenes appended with thioamide moieties as powerful tool for heavy metals recognition
PublicationSelectivity of new thioamide derivatives was assessed using those ligands as sensor materials in ion-selective membrane electrodes and tested towards Pb2+ - selectivity. The influence of the nature of the thioamide function (linear, branched or cyclic substituents) on their ionophoric properties was investigated. Electrodes based on cyclic thioamide moieties are promising analytical tools for monitoring Pb2+ concentration in natural...
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Calix[4]arene-Thioamides as Ionophores for Transition and Heavy Metal cations
PublicationCalix[4]arene derivatives play an important role as sensing materials in Ion Selective Electrodes(ISEs). Nowadays a high impact is put to control in natural waters the level of toxic heavy metals, like Pb ,Cd, Hg or Cu which may cause the great risk to human health. Our goal was to design and to synthesize ligands possessing ability to bind transition and heavy metal cations. The synthesis, crystal structures,extractive and ionophoric...
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Recognition and sensing of anions
PublicationMolecular ion recognition is one of the most intensively studied areas of supramolecular technology. The reason for this is the essential role that ions play in many biological as well as industrial processes. On the other hand, however, it has been proved that ions can have a negative impact on human health and the environment. For these reasons, it is extremly important to develop rapid and simple methods allowing the determination...
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Imidazoacridinone antitumor agent C-1311 as a selective mechanism- based inactivator of human cytochrome P450 1A2 and 3A4 isoenzymes.
Publication5-Diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311), a promising antitumor agent that is also active against autoimmune diseases, was determined to be a selective inhibitor of the cytochrome P450 (CYP) 1A2 and 3A4 isoenzymes. Therefore, C-1311 might modulate the effectiveness of other drugs used in multidrug therapy. The present work aimed to identify the mechanism of the observed C-1311-mediated inactivation of CYP1A2...
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Chromogenic amides of pyridine-2,6-dicarboxylic acid as anion receptors
PublicationThe synthesis of simple, chromogenic pyridine-2,6-dicarboxylic acid amides, derivates of isomeric nitroanilines and aminonitrophenols, and their ion binding properties are described. The ligands' response to ionic species was examined by naked eye and was studied with the use of UV-Vis spectroscopy in DMSO and its mixture with water. The effect of the localisation and the type of the substituents in aromatic rings were discussed....
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Novel anticancer strategy aimed at targeting shelterin complexes by the induction of structural changes in telomeric DNA: hitting two birds with one stone.
PublicationThe ends of chromosomes in mammals are composed of telomeric DNA containing TTAGGG repeats, which bind specific proteins called shelterins. This telomeric DNA together with shelterins form a cap that protects the ends of chromosomes from being recognized as sites of DNA damage and from chromosomal fusions. Many very successful antitumor drugs used in the treatment of cancer patients bind to DNA, some of them with a prominent sequence...
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HDAC Inhibitors: Innovative Strategies for Their Design and Applications
PublicationHistone deacetylases (HDACs) are a large family of epigenetic metalloenzymes that are involved in gene transcription and regulation, cell proliferation, differentiation, migration, and death, as well as angiogenesis. Particularly, disorders of the HDACs expression are linked to the development of many types of cancer and neurodegenerative diseases, making them interesting molecular targets for the design of new efficient drugs...