2127-05-1Relevant articles and documents
On the pH-Modulated Ru-Based Prodrug Activation Mechanism
Caterino, Marco,Herrmann, Mona,Merlino, Antonello,Riccardi, Claudia,Montesarchio, Daniela,Mroginski, Maria A.,Musumeci, Domenica,Ruffo, Francesco,Paduano, Luigi,Hildebrandt, Peter,Kozuch, Jacek,Vergara, Alessandro
supporting information, p. 1216 - 1223 (2019/01/26)
The RuIII-based prodrug AziRu efficiently binds to proteins, but the mechanism of its release is still disputed. Herein, in order to test the hypothesis of a reduction-mediated Ru release from proteins, a Raman-assisted crystallographic study on AziRu binding to a model protein (hen egg white lysozyme), in two different oxidation states, RuII and RuIII, was carried out. Our results indicate Ru reduction, but the Ru release upon reduction is dependent on the reducing agent. To better understand this process, a pH-dependent, spectroelectrochemical surface-enhanced Raman scattering (SERS) study was performed also on AziRu-functionalized Au electrodes as a surrogate and simplest model system of RuII- and RuIII-based drugs. This SERS study provided a pKa of 6.0 ± 0.4 for aquated AziRu in the RuIII state, which falls in the watershed range of pH values separating most cancer environments from their physiological counterparts. These experiments also indicate a dramatic shift of the redox potential E0 by >600 mV of aquated AziRu toward more positive potentials upon acidification, suggesting a selective AziRu reduction in cancer lumen but not in healthy ones. It is expected that the nature of the ligands (e.g., pyridine vs imidazole, present in well-known RuIII complex NAMI-A) will modulate the pKa and E0, without affecting the underlying reaction mechanism.
PROCESS FOR PREPARING BISPHENOL
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Page/Page column 27-28, (2011/12/12)
Provided is a process for producing a bisphenol compound stably at a high conversion and with high selectivity over a long period. A process for producing a bisphenol compound by feeding a phenol compound and a carbonyl compound continuously to a reactor packed with an acid catalyst, characterized in that the acid catalyst is a sulfonic-acid-form cation-exchange resin in which part of the sulfo groups have been modified with at least any one of 2-pyridylalkanethiol compounds and 3-pyridylalkanethiol compounds.
Process for producing 2-(4-pyridyl)ethanethiol
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, (2008/06/13)
An object of the present invention is to provide a process for producing 2-(4-pyridyl)ethanethiol easily. According to the invention, 4-vinylpyridine is reacted with thiourea in an aqueous medium containing an acid to form a solution containing an isothiuronium salt and then the solution is made alkaline to convert the isothiuronium salt into 2-(4-pyridyl)ethanethiol.