- Charge neutral rhenium tricarbonyl complexes of tridentate N-heterocyclic carbene ligands that bind to amyloid plaques of Alzheimer's disease
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Two tridentate ligand systems bearing N-heterocyclic carbene (NHC), amine and carboxylate donor groups coupled to benzothiazole- or stilbene-based amyloid binding moieties were synthesised. Reaction of the imidazolium salt containing pro-ligands with Re(CO)5Cl yielded the corresponding rhenium metal complexes which were characterised by NMR, and X-ray crystallography. These ligands are of interest for the potential preparation of technetium-99m imaging agents for Alzheimer's disease and the capacity of these rhenium complexes bind to amyloid fibrils composed of amyloid-β peptide and amyloid plaques in human frontal cortex brain tissue was evaluated using fluorescence microscopy. These studies show that the complexes bound efficiently to amyloid-β fibrils and some evidence of binding to amyloid-β plaques.
- Barnard, Peter J.,Donnelly, Paul S.,McLean, Catriona A.,Noor, Asif,Wiratpruk, Nuchareenat
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p. 4559 - 4569
(2020/04/17)
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- Facile Access to the 12-Membered Macrocyclic Ligand PCTA and Its Derivatives with Carboxylate, Amide, and Phosphinate Ligating Functionalities
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We describe a convenient synthetic pathway to access the 12-membered PCTA macrocycle, a polyaminocarboxylate ligand for which its M2+ and M3+ complexes are commonly associated with applications in biomedical diagnostics and radiother
- Enel, Morgane,Leygue, Nadine,Saffon, Nathalie,Galaup, Chantal,Picard, Claude
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supporting information
p. 1765 - 1773
(2018/04/27)
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- Stable Europium(III) Complexes with Short Linkers for Site-Specific Labeling of Biomolecules
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In this study, two new terpyridine-based EuIII complexes were synthesized, the structures of which were optimized for luminescence resonance energy-transfer (LRET) experiments. The complexes showed high quantum yields (32 %); a single long life
- Faschinger, Felix,Ertl, Martin,Zimmermann, Mirjam,Horner, Andreas,Himmelsbach, Markus,Sch?fberger, Wolfgang,Kn?r, Günther,Gruber, Hermann J.
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p. 721 - 732
(2017/12/12)
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- Bimodal ligands with macrocyclic and acyclic binding moieties, complexes and compositions thereof, and methods of using
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Substituted 1,4,7-triazacyclononane-N,N′,N″-triacetic acid and 1,4,7,10-tetraazacyclcododecane-N,N′,N″,N′″-tetraacetic acid compounds with a pendant amino or hydroxyl group, metal complexes thereof, compositions thereof, and methods of making and use in diagnostic imaging and treatment of cellular disorders.
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- Ring expansion of 2-(1-Hydroxyalkyl)azetidines to 4-(2-Chloroethyl) oxazolidinones
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2-(1-Hydroxyalkyl)azetidines react with bis(trichloromethyl) carbonate (BTC) after basic treatment to afford 4-(2-chloroethyl)oxazolidinones. The scope of this rearrangement was examined in detail and its efficiency was shown to depend on the class of the
- Couty, Francois,Drouillat, Bruno,Lemee, Frederic
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experimental part
p. 794 - 801
(2011/03/22)
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- Polyazamacrocycles based on a tetraaminoacetate moiety and a (poly)pyridine intracyclic unit: Direct synthesis and application to the photosensitization of Eu(III) and Tb(III) ions in aqueous solutions
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A series of five new 15-, 18- or 21-membered polyazamacrocycles (L 1-L5) based on a pyridine, bipyridine or terpyridine unit and a triethylenetetraminetetraacetic acid (TTTA) skeleton is described. In ligands L4 and L
- Bechara, Ghassan,Leygue, Nadine,Galaup, Chantal,Mestre-Voegtlé, Béatrice,Picard, Claude
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experimental part
p. 8594 - 8604
(2011/01/04)
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- An efficient route to pyridine and 2,2'-bipyridine macrocycles incorporating a triethylenetetraminetetraacetic acid core as ligand for lanthanide ions
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Two novel macrocyclic chelators L1 and L2 incorporating an intracyclic pyridine or 2,2'-bipyridine unit and a triethylenetetraminetetraacetic acid core (TTTA) were synthesized with the aim of forming lanthanide complexes suitable as
- Bechara, Ghassan,Leygue, Nadine,Galaup, Chantal,Mestre, Béatrice,Picard, Claude
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scheme or table
p. 6522 - 6525
(2011/02/24)
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- Synthesis and evaluation of novel polyaminocarboxylate-based antitumor agents
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Iron depletion, using iron chelators targeting transferrin receptor (TfR) and ribonucleotide reductase (RR), is proven to be effective in the treatment of cancer. We synthesized and evaluated novel polyaminocarboxylate-based chelators NETA, NE3TA, and NE3TA-Bn and their bifunctional versions C-NETA, C-NE3TA, and N-NE3TA for use in iron depletion tumor therapy. The cytotoxic activities of the novel polyaminocarboxylates were evaluated in the HeLa and HT29 colon cancer cell lines and compared to the clinically available iron depletion agent DFO and the frequently explored polyaminocarboxylate DTPA. All new chelators except C-NETA displayed enhanced cytotoxicities in both HeLa and HT29 cancer cells compared to DFO and DTPA. Incorporation of the nitro functional unit for conjugation to a targeting moiety into the two potent non-functionalized chelators NE3TA and NE3TA-Bn (C-NE3TA and N-NE3TA) was well-tolerated and resulted in a minimal decrease in cytotoxicity. Cellular uptake of C-NE3TA, examined using a confocal microscope, indicates that the chelator is taken up into HT29 cancer cells.
- Chong, Hyun-Soon,Ma, Xiang,Lee, Haisung,Bui, Phuong,Song, Hyun A.,Birch, Noah
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p. 2208 - 2215
(2008/12/21)
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- Multiply substituted DTPA derivatives and their metal complexes, and their metal complexes, pharmaceutical agents that contain these complexes, their use in diagnosis and therapy, as well as process for the production of pharmaceutical agents
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The invention relates to new, multiply substituted diethylenetriaminepentaacetic acid derivatives, their complexes and complex salts, that contain an element of atomic numbers 20-32, 39-51 or 57-83, pharmaceutical agents that contain these compounds, their use as contrast media and antidotes, and process for the production of pharmaceutical agents.
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- Nucleic acid-binding oligomers possessing N-branching for therapy and diagnostics
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The invention relates to nucleic acid-binding oligomers possessing N-branching of the general formula (I), STR1 and their monomers, where the individual radicals have the meaning given in the description, and to their use as medicaments or as aids in diag
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