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排序方式: 共有587条查询结果,搜索用时 31 毫秒
91.
Dimitrios Vagiannis Youssif Budagaga Anselm Morell Yu Zhang Eva Novotn Adam Skarka Sarah Kammerer Jan-Heiner Küpper Ivo Hanke Tom Rozko Jakub Hofman 《International journal of molecular sciences》2021,22(21)
Tepotinib is a novel tyrosine kinase inhibitor recently approved for the treatment of non-small cell lung cancer (NSCLC). In this study, we evaluated the tepotinib’s potential to perpetrate pharmacokinetic drug interactions and modulate multidrug resistance (MDR). Accumulation studies showed that tepotinib potently inhibits ABCB1 and ABCG2 efflux transporters, which was confirmed by molecular docking. In addition, tepotinib inhibited several recombinant cytochrome P450 (CYP) isoforms with varying potency. In subsequent drug combination experiments, tepotinib synergistically reversed daunorubicin and mitoxantrone resistance in cells with ABCB1 and ABCG2 overexpression, respectively. Remarkably, MDR-modulatory properties were confirmed in ex vivo explants derived from NSCLC patients. Furthermore, we demonstrated that anticancer effect of tepotinib is not influenced by the presence of ABC transporters associated with MDR, although monolayer transport assays designated it as ABCB1 substrate. Finally, tested drug was observed to have negligible effect on the expression of clinically relevant drug efflux transporters and CYP enzymes. In conclusion, our findings provide complex overview on the tepotinib’s drug interaction profile and suggest a promising novel therapeutic strategy for future clinical investigations. 相似文献
92.
Willi Kantlehner Markus Vettel Hansjrg Lehmann Kai Edelmann Rüdiger Stieglitz Ivo C. Ivanov 《Advanced Synthesis \u0026amp; Catalysis》1998,340(5):408-423
Orthoamides. LI. Push-Pull-Butadienes and Heterocycles from Alkyne Carboxylic Acid Orthoamides and CH2-acidic Compounds The acetylides 4b, 4f react with N,N,N′,N′,N″,N″-hexamethylguanidiniumchloride ( 5 ) to give the orthoamides 6b, 6f , resp. From CH2-acidic compounds and the orthoamides 6a, c, e can be obtained the push-pull-substituted butadienes 8a–8aj . The 2,3,5-trimethyl-thiadiazolium salt 9 does not condense with 6e , as other CH2-acidic compounds do, instead the vinylogous guanidinium salt 10a is produced. On heating, the ketenaminals 8d, aa cyclize to give the pyridone-carbonitriles 11a, b , resp. From 4-amino-coumarins 12 and the orthocarboxylic acid amideacetals 13a, b and the ketenaminal 16 resp., the amidines 14a–c and the heterocyclic compounds 15a–c resp., are formed. The enamines 17a–c, 19a, b react with the orthoamides 6a–f to give the pyridine derivatives 18a–1, 20a–h and 21a, b , resp. Analogously, from 6-aminouracil 22 and 6a, b, e, f are formed the pure 7-dimethylaminopyrido[2,3-d] pyrimidines 23a, b or mixtures of compounds 23c, d and the isomeric 4-dimethylamino-pyrido[2,3-d]pyrimidines 24a, b resp., which can be separated via their salts 25a,b/26a,b . The heterocyclic compounds 30a–d, 32a,b can be prepared from the pyrazole derivatives 28, 31 resp. and the orthoamides 6a–f . 相似文献
93.
The copolymerization of acrylonitrile with two polymerizable fluorescent naphthalimide dyes has been investigated. It was found that the monomeric dyes took part in the polymerization and 94–96% of initially 1 wt.-% (relative to acrylonitrile) were covalently bound in the polymer chain, and thus new fluorescent side-group copolymers were obtained. The absorption and basic photophysical characteristics of monomeric naphthalimid dyes and copolymers in dimethylformamide are reported. 相似文献
94.
A. Glover Bailie Karel Bouzek Petr Lukek Ivo Rouar Anthony A. Wragg 《Journal of chemical technology and biotechnology (Oxford, Oxfordshire : 1986)》1996,66(1):35-40
The solubility of potassium ferrate (K2FeO4) was measured in aqueous solutions of NaOH and KOH of total concentration 12 M containing various molar ratios of KOH:NaOH in the range 12:0 to 3:9. Several analytical methods were tested for the determination of ferrate concentration. The final method chosen consisted of potentiometric titration of the ferrate sample with an alkaline solution of As2O3. The assumption was made that ferrate dissociates in concentrated KOH solutions predominantly to KFeO4−. The solubility constant, S, defined as the product of the molar concentration of the potassium ion, K+, and the ferrate anion, KFeO4−, was found to be 0·044 ± 0·006 mol2 dm−6 for 20°C, 0·093 ± 0·004 mol2 dm−6 for 40°C and 0·15 ± 0·09 mol2 dm−6 for 60°C. From these results the heat of dissolution of K2FeO4 was calculated as −14·3 kJ mol−1. At 60°C the enhanced decomposition of the ferrate at the higher temperature led to a greater deviation in solubility values compared with data for either 20°C or 40°C. 相似文献
95.
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98.
Messai A. Mamo Alan O. Sustaita Zikhona N. Tetana Neil J. Coville Ivo A. Hümmelgen 《Journal of Materials Science: Materials in Electronics》2013,24(10):3995-4000
We report on hydrostatic pressure sensors prepared using 10 % w/w multiwalled carbon nanotube (MWCNT)/poly(vinyl alcohol) composites. Three types of carbon nanotubes were used in the composites: undoped MWCNTs, nitrogen-doped MWCNTs and boron-doped MWCNTs (B-MWCNTs). The sensor response was tested using an alternating current input, measuring the capacitance and conductance outputs. The sensors based on the three composites show a linear capacitance and conductance sensitivity pressure dependence in the range 50–120 kPa, but a higher sensitivity to pressure dependence above this interval. The highest angular coefficient of the sensitivity, which reached 0.092 kPa?1, was observed for the capacitance sensitivity of the B-MWCNT based composite. 相似文献
99.
100.
Tsermaa Galya Vladimír Sedlařík Ivo Kuřitka Radko Novotný Jana Sedlaříková Petr Sáha 《应用聚合物科学杂志》2008,110(5):3178-3185
The importance of antibacterial materials for biomedical applications is growing nowadays. The presented article deals with the characterization of structural, mechanical and thermal properties and of antibacterial polymeric films based on polyvinyl alcohol (PVA) and silver nitrate, which can find their applicability in wound dressing components and protective coating. The methods of transmission electron microscopy, UV–vis and XRD spectroscopy, optical microscopy, differential scanning calorimetry, stress–strain analysis, and agar diffusion test were used to characterize the polymer films prepared. The results showed strong antibacterial activity against Escherichia coli and Staphylococcus aureus already at the lowest addition level of silver nitrate. An improvement of mechanical properties (Young's modulus) was also noticed due to a modification of PVA with silver nitrate up to 1 wt. % of silver content. Furthermore, the results show a strong effect of the thermal history of the sample preparation on the degree of silver‐ion reduction and formation of nanoparticles. © 2008 Wiley Periodicals, Inc. J Appl Polym Sci, 2008 相似文献