- Polyviologen synthesis by self-assembly assisted grafting
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In this work a new method for electrochemical polymerization of a viologen derivative is presented. A precursor, having an isothiocyanate group as a "head"-group and a cyanopyridine group as a "tail"-group (SCNCP), suitable for self-assembly was designed
- Wang, Nianxing,K?hk?nen, Anniina,??ritalo, Timo,Damlin, Pia,Kankare, Jouko,Kvarnstr?m, Carita
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p. 101232 - 101240
(2015)
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- Design, synthesis, computational, and preclinical evaluation of Natti/45Ti-labeled urea-based glutamate PSMA ligand
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Despite promising anti-cancer properties in vitro, all titanium-based pharmaceuticals have failed in vivo. Likewise, no target-specific positron emission tomography (PET) tracer based on the radionuclide 45Ti has been developed, notwithstanding its excellent PET imaging properties. In this contribution, we present liquid–liquid extraction (LLE) in flow-based recovery and the purification of 45Ti, computer-aided design, and the synthesis of a salan-natTi/45Ti-chelidamic acid (CA)-prostate-specific membrane antigen (PSMA) ligand containing the Glu-urea-Lys pharmacophore. The compound showed compromised serum stability, however, no visible PET signal from the PC3+ tumor was seen, while the ex vivo biodistribution measured the tumor accumulation at 1.1% ID/g. The in vivo instability was rationalized in terms of competitive citrate binding followed by Fe(III) transchelation. The strategy to improve the in vivo stability by implementing a unimolecular ligand design is presented.
- Baun, Christina,Jensen, Andreas Ingemann,Nielsen, Karin Michaelsen,Pedersen, Kristina S?borg,Thisgaard, Helge,Zhuravlev, Fedor
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- NOVEL BENZOTHIAZEPINE AND BENZOTHIEPINE COMPOUNDS
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A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis an
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- Syntheses of Reactive Fluorescent Stains Derived from 5(2)-Aryl-2(5)-(4-pyridyl)oxazoles and Bifunctionally Reactive Linkers
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Several bifunctionally reactive linkers containing halide or sulfonate ester groups were prepared.The linkers were used to quaternize 5-(4-methoxyphenyl)-2-(4-pyridyl)oxazole and 2-(6-chromanyl)-5-(4-pyridyl)oxazole to produce fluorescent stains that contained a reactive group such as an isothiocyanate, an N-hydroxysuccinimidyl ester, a maleimide, or an oxirane.The stains were derivatized with either 1-propyl-amine, 1-propanethiol, or piperidine, as appropriate, to help in characteriazation.The stains may serve as more photostable alternatives to fluoresceins or coumarins.
- Litak, Peter T.,Kauffman, Joel M.
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p. 457 - 480
(2007/10/02)
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