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排序方式: 共有868条查询结果,搜索用时 15 毫秒
861.
Jerneja Kladnik Dr. Jakob Kljun Hilke Burmeister Prof. Dr. Ingo Ott Dr. Isolda Romero-Canelón Prof. Dr. Iztok Turel 《Chemistry (Weinheim an der Bergstrasse, Germany)》2019,25(62):14169-14182
An organoruthenium(II) complex with pyrithione (2-mercaptopyridine N-oxide) 1 a has previously been identified by our group as a compound with promising anticancer potential without cytotoxicity towards non-cancerous cells. To expand the rather limited research on compounds of this type, an array of novel chlorido and 1,3,5-triaza-7-phosphaadamantane (pta) organoruthenium(II) complexes with methyl-substituted pyrithiones has been prepared. After thorough investigation of the aqueous stability of these complexes, their modes of action have been elucidated at the cellular level. Minor structural alterations in the ruthenium-pyrithionato compounds resulted in fine-tuning of their cytotoxicities. The best performing compounds, 1 b and 2 b , with a chlorido or pta ligand bound to ruthenium, respectively, and a methyl group at the 3-position of the pyrithione scaffold, have been further investigated. Both compounds trigger early apoptosis, induce the generation of reactive oxygen species and G1 arrest in A549 cancer cells, and show no strong interaction with DNA. However, only 1 b also inhibits thioredoxin reductase. Wound healing assays and mitochondrial function evaluation have revealed differences between these two compounds at the cellular level. 相似文献
862.
Eduard Badarau Frédéric Robert Stéphane Massip Florian Jakob Simon Lucas Sven Frormann Léon Ghosez 《Tetrahedron》2018,74(38):5119-5128
Spirocyclic indazoles were designed as potential ligands for the glucocorticoid receptors (GRs). A short and efficient synthetic sequence was developed allowing the preparation of pure diastereomeric spirocyclic analogs of fluorocortivazol. Our studies also revealed a new application of Burgess reagent leading to a ring expansion. The structures and conformations of several key intermediates and products were confirmed by single crystal X-ray diffraction analysis. Conformational assignments were also supported by DFT calculations. As a proof of concept we tested the affinity of diastereomeric compounds 13b and 14b for the GRs. Rewardingly, it was found that 14b showed a promising IC50 of 27?nM. 相似文献
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The partial wave crossing relations derived in a recent paper by Steiner [1] are used for a calculation of the πN S-wave amplitudes in the region 8 ≦ s ≦ (M − 1)2. The corresponding Argand diagrams show the pseudoresonance behaviour predicted in [1]. The results for the real parts are compared with an independent calculation using fixed-t dispersion relations. 相似文献
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867.
Nara Altmann Peter J. Halley Justin Cooper‐White Jakob Lange 《Macromolecular Symposia》2001,169(1):171-177
Highly filled thermosets are used in applications such as integrated circuit (IC) packaging. However, a detailed understanding of the effects of the fillers on the macroscopic cure properties is limited by the complex cure of such systems. This work systematically quantifies the effects of filler content on the kinetics, gelation and vitrification of a model silica‐filled epoxy/amine system in order to begin to understand the role of the filler in IC packaging cure. At high cure temperatures (100°C and above) there appears to be no effect of fillers on cure kinetics and gelation and vitrification times. However, a decrease in the gelation and vitrification times and increase the reaction rate is seen with increasing filler content at low cure temperatures (60‐90°C). An explanation for these results is given in terms of catalysation of the epoxy amine reaction by hydrogen donor species present on the silica surface and interfacial effects. 相似文献
868.