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排序方式: 共有1186条查询结果,搜索用时 18 毫秒
61.
62.
Dr. Qaisar Nadeem Dr. Federica Battistin Dr. Olivier Blacque Prof. Dr. Roger Alberto 《Chemistry (Weinheim an der Bergstrasse, Germany)》2022,28(5):e202103566
Bis-arene sandwich complexes are generally prepared by the Fischer-Hafner reaction, which conditions are incompatible with most O- and N- functional groups. We report a new way for the synthesis of sandwich type complexes [Re(η6-arene)2]+ and [Re(η6-arene)(η6-benzene)]+ from [Re(η6-napht)2]+ and [Re(η6-napht)(η6-benzene)]+, with functionalized arenes and pharmaceuticals. N-methylpyrrolidine (NMP) facilitates the substitution of naphthalene with the incoming arene. A series of fully characterized rhenium sandwich complexes with simple arenes, such as aniline, as well as with active compounds like lidocaine and melatonin are presented. With these rhenium compounds in hand, the radioactive sandwich complexes [99mTc(η6-pharm)2]+ (pharm=pharmaceutical) can be unambiguously confirmed. The direct labelling of pharmaceuticals with 99mTc through η6-coordination to phenyl rings and the confirmation of the structures with the rhenium homologues opens a path into molecular theranostics. 相似文献
63.
64.
If the baryon asymmetry of the Universe is produced by leptogenesis, CP violation is required in the lepton sector. In the seesaw extension of the standard model with three hierarchical right-handed neutrinos, we show that the baryon asymmetry is insensitive to the Pontecorvo-Maki-Nagakawa-Sakata phases: thermal leptogenesis can work for any value of the observable phases. This result was well known when there were no flavor effects in leptogenesis; we show that it remains true when flavor effects are included. 相似文献
65.
Laredo E Prutsky N Bello A Grimau M Castillo RV Müller AJ Dubois P 《The European physical journal. E, Soft matter》2007,23(3):295-303
Thermally stimulated depolarization currents, TSDC, wide-angle X-ray scattering, WAXS, differential scanning calorimetry,
DSC, and polarized light optical microscopy, PLOM, have been used to examine poly(L-lactide)-b -poly(
-caprolactone) diblock copolymers in a wide composition range. Both components are crystallizable and the miscibility in
the amorphous phase has been determined from the behavior of the primary relaxations which are the dielectric manifestation
of the glass transition, and also from the superstructural morphology revealed by PLOM and the compositional dependence of
the melting points as determined by DSC. Distinct segmental mobilities in the amorphous phase which can be well resolved by
TSDC are present; the
mode of the slower component shifts to lower temperatures as the PCL content increases while the glass transition of neat
PCL is present for all compositions. A relaxation times bimodal distribution is apparent for PCL-rich copolymers. The composition
dependence of the multiple glass transitions detected in these weakly segregated copolymers are predicted by the self-concentration
model for a miscible blend made of components with a large Tg contrast. 相似文献
66.
Dr. Elisa Bonandi Dr. Mattia Mori Dr. Paola Infante Dr. Irene Basili Prof. Dr. Lucia Di Marcotullio Dr. Andrea Calcaterra Dr. Federica Catti Prof. Dr. Bruno Botta Prof. Dr. Daniele Passarella 《Chemistry (Weinheim an der Bergstrasse, Germany)》2021,27(32):8350-8357
Withanolides constitute a well-known family of plant-based alkaloids characterised by widespread biological properties, including the ability of interfering with Hedgehog (Hh) signalling pathway. Following our interest in natural products and in anticancer compounds, we report here the synthesis of a new class of Hh signalling pathway inhibitors, inspired by withaferin A, the first isolated member of withanolides. The decoration of our scaffolds was rationally supported by in silico studies, while functional evaluation revealed promising candidates, confirming once again the importance of natural products as inspiration source for the discovery of novel bioactive compounds. A stereoselective approach, based on Brown chemistry, allowed the obtainment and the functional evaluation of the enantiopure hit compounds. 相似文献
67.
HPLC‐MS/MS method for quantitative determination of the novel dual inhibitor of FGF and VEGF receptors E‐3810 in tumor tissues from xenograft mice and human biopsies 下载免费PDF全文
Monique Zangarini Laura Ceriani Ezia Bello Giovanna Damia Roberta Cereda Maria Gabriella Camboni Massimo Zucchetti 《Journal of mass spectrometry : JMS》2014,49(1):19-26
We developed and validated a high‐performance liquid chromatography–tandem mass spectrometry analytical method to measure E‐3810, a novel dual inhibitor of fibroblast growth factor receptor 1 and vascular endothelial growth factor receptor 1–3 in tissues and determined the drug concentration in a biopsy of human breast cancer for the first time. The method is a modification of our previous one in plasma to study the clinical pharmacokinetics of the drug during the phase I/II trial. In view of the changes in matrix, we applied a partial validation protocol to determine recovery, sensitivity, range of linearity, precision, accuracy and stability of the method over three runs in a mouse tumor tissue and liver. The recovery of E‐3810 from liver or tumor homogenate was >69%, and the lower limit of quantification was 5 ng/ml. The method was linear in the concentration range 5.0–500.0 ng/ml, as demonstrated by a determination coefficient R2 ≥ 0.9955. The range of the calibration curve was appropriate for the analysis, as demonstrated by the accuracy, which was between 91.4% and 106.7%. Interday precision and accuracy on quality control samples at 9, 30 and 300 ng/ml were 3.1‐11.2% and 98.3–111.4%, respectively. The assay was applied successfully to determine the intratumor concentration of E‐3810 in different mouse xenograft tumor models and in a biopsy of a patient with breast cancer included in the phase I/II trial of the drug. In mouse tumors, the concentrations of E‐3810 were higher than necessary to exert antitumor activity in vitro (1 µM). Even more of interest was the result obtained in a human biopsy of few milligrams, where E‐3810 reached 4.9 µg/g (11 µM). Copyright © 2014 John Wiley & Sons, Ltd. 相似文献
68.
Cell Tracking with Caged Xenon: Using Cryptophanes as MRI Reporters upon Cellular Internalization 下载免费PDF全文
Stefan Klippel Jörg Döpfert Dr. Jabadurai Jayapaul Martin Kunth Federica Rossella Matthias Schnurr Dr. Christopher Witte Dr. Christian Freund Dr. Leif Schröder 《Angewandte Chemie (International ed. in English)》2014,53(2):493-496
Caged xenon has great potential in overcoming sensitivity limitations for solution‐state NMR detection of dilute molecules. However, no application of such a system as a magnetic resonance imaging (MRI) contrast agent has yet been performed with live cells. We demonstrate MRI localization of cells labeled with caged xenon in a packed‐bed bioreactor working under perfusion with hyperpolarized‐xenon‐saturated medium. Xenon hosts enable NMR/MRI experiments with switchable contrast and selectivity for cell‐associated versus unbound cages. We present MR images with 103‐fold sensitivity enhancement for cell‐internalized, dual‐mode (fluorescence/MRI) xenon hosts at low micromolar concentrations. Our results illustrate the capability of functionalized xenon to act as a highly sensitive cell tracer for MRI detection even without signal averaging. The method will bridge the challenging gap for translation to in vivo studies for the optimization of targeted biosensors and their multiplexing applications. 相似文献
69.
Back Cover: Cell Tracking with Caged Xenon: Using Cryptophanes as MRI Reporters upon Cellular Internalization (Angew. Chem. Int. Ed. 2/2014) 下载免费PDF全文
70.
Luisa Pieroni Federica Iavarone Alessandra Olianas Viviana Greco Claudia Desiderio Claudia Martelli Barbara Manconi Maria Teresa Sanna Irene Messana Massimo Castagnola Tiziana Cabras 《Journal of separation science》2020,43(1):313-336
More than 300 different protein post‐translational modifications are currently known, but only a few have been extensively investigated because modified proteoforms are commonly present in sub‐stoichiometry amount. For this reason, improvement of specific enrichment techniques is particularly useful for the proteomic characterization of post‐translationally modified proteins. Enrichment proteomic strategies could help the researcher in the challenging issue to decipher the complex molecular cross‐talk existing between the different factors influencing the cellular pathways. In this review the state of art of the platforms applied for the enrichment of specific and most common post‐translational modifications, such as glycosylation and glycation, phosphorylation, sulfation, redox modifications (i.e. sulfydration and nitrosylation), methylation, acetylation, and ubiquitinylation, are described. Enrichments strategies applied to characterize less studied post‐translational modifications are also briefly discussed. 相似文献