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1.
Pan-Gyn cancers entail 1 in 5 cancer cases worldwide, breast cancer being the most commonly diagnosed and responsible for most cancer deaths in women. The high incidence and mortality of these malignancies, together with the handicaps of taxanes—first-line treatments—turn the development of alternative therapeutics into an urgency. Taxanes exhibit low water solubility that require formulations that involve side effects. These drugs are often associated with dose-limiting toxicities and with the appearance of multi-drug resistance (MDR). Here, we propose targeting tubulin with compounds directed to the colchicine site, as their smaller size offer pharmacokinetic advantages and make them less prone to MDR efflux. We have prepared 52 new Microtubule Destabilizing Sulfonamides (MDS) that mostly avoid MDR-mediated resistance and with improved aqueous solubility. The most potent compounds, N-methyl-N-(3,4,5-trimethoxyphenyl-4-methylaminobenzenesulfonamide 38, N-methyl-N-(3,4,5-trimethoxyphenyl-4-methoxy-3-aminobenzenesulfonamide 42, and N-benzyl-N-(3,4,5-trimethoxyphenyl-4-methoxy-3-aminobenzenesulfonamide 45 show nanomolar antiproliferative potencies against ovarian, breast, and cervix carcinoma cells, similar or even better than paclitaxel. Compounds behave as tubulin-binding agents, causing an evident disruption of the microtubule network, in vitro Tubulin Polymerization Inhibition (TPI), and mitotic catastrophe followed by apoptosis. Our results suggest that these novel MDS may be promising alternatives to taxane-based chemotherapy in chemoresistant Pan-Gyn cancers.  相似文献   
2.
Over the last few years, the global biosurfactant market has raised due to the increasing awareness among consumers, for the use of biological or bio-based products. Because of their composition, it can be speculated that these are more biocompatible and more biodegradable than their chemical homologous. However, at the moment, no studies exist in the literature about the biodegradability of biosurfactants. In this work, a biosurfactant contained in a crude extract, obtained from a corn wet-milling industry stream that ferments spontaneously in the presence of lactic acid bacteria, was subjected to a biodegradation study, without addition of external microbial biomass, under different conditions of temperature (5–45 °C), biodegradation time (15–55 days), and pH (5–7). For that, a Box–Behnken factorial design was applied, which allowed to predict the percentage of biodegradation for the biosurfactant contained in the crude extract, between the range of the independent variables selected in the study, obtaining biodegradation values between 3 and 80%. The percentage of biodegradation for the biosurfactant was calculated based on the increase in the surface tension of samples of the crude extract. Furthermore, it was also possible to predict the variation in t1/2 for the biosurfactant (time to achieve the 50% of biodegradation) under different conditions.  相似文献   
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4.
Since fullerenes and carbon nanotubes (CNTs) were discovered, these materials have attracted a great deal of attention in the scientific community due to their unique structures and properties. The properties of both carbon allotropes can be modulated by chemical functionalization, and merging fullerenes and CNTs combines the electronic and optical properties of CNTs with the excellent electron acceptor characteristic of fullerenes; moreover, a synergistic effect of these hybrids can be found, as the properties of both the nanotube and the fullerene are affected by the presence of the other. In these hybrids, the fullerene can be located inside (endohedral) or outside (exohedral) the CNT and both types of hybrid have specific features. CNT-fullerene hybrids have been studied for various applications, including photovoltaics, optical limiting and flame retardancy amongst others. This review outlines the progress in research on CNT-fullerene hybrids, including endohedral and exohedral combinations, their properties, functionalization, applications and outlook.  相似文献   
5.
Compared to traditional vacuum evaporation techniques for small organic molecules, organic vapor phase deposition (OVPD) possesses a extra processing parameter: the pressure of process gas Pch. Here, the influence of large Pch variations (from 0.1 mbar to atmospheric pressure) on pentacene thin film growth is explored. OVPD operation at higher Pch is characterized by lower carrier gas velocities and lower organic diffusivities. These result in an invariance of the material utilization efficiency over the entire pressure span and in an advantageous equilibrium evaporation regime in the source. An increase in Pch yields rough pentacene layers. Classical nucleation theory is applied to demonstrate how the pressure rise triggers homogeneous nucleation in the gas phase, causing the observed roughening. The use of lower deposition rates, higher dilution flow rates, and higher substrate temperatures result in the suppression of gas phase nucleation and the growth of smooth pentacene films at atmospheric pressure. Using these optimized conditions, state‐of‐the‐art pentacene thin film transistors with saturation mobilities above 0.9 cm2/Vs are reproducibly fabricated. p‐Type circuits are also made and a 19‐stage ring oscillator with a stage delay of 51 μs at a supply voltage of 15 V is demonstrated.  相似文献   
6.

Abstract  

Samarium diiodide is an efficient catalyst for the aminolysis of either activated or non activated aziridines with aromatic amines. A variety of N-diprotected β-diamines has been prepared including new products. The comparison of the N-protecting groups of aziridines in reactions catalyzed by samarium diiodide or by samarium iodobinaphtholate indicates that N-Boc protection leads to the best results.  相似文献   
7.
A pattern is a model or a template used to summarize and describe the behavior (or the trend) of data having generally some recurrent events. Patterns have received a considerable attention in recent years and were widely studied in the data mining field. Various pattern mining approaches have been proposed and used for different applications such as network monitoring, moving object tracking, financial or medical data analysis, scientific data processing, etc. In these different contexts, discovered patterns were useful to detect anomalies, to predict data behavior (or trend) or, more generally, to simplify data processing or to improve system performance. However, to the best of our knowledge, patterns have never been used in the context of Web archiving. Web archiving is the process of continuously collecting and preserving portions of the World Wide Web for future generations. In this paper, we show how patterns of page changes can be useful tools to efficiently archive Websites. We first define our pattern model that describes the importance of page changes. Then, we present the strategy used to (i) extract the temporal evolution of page changes, (ii) discover patterns, to (iii) exploit them to improve Web archives. The archive of French public TV channels France Télévisions is chosen as a case study to validate our approach. Our experimental evaluation based on real Web pages shows the utility of patterns to improve archive quality and to optimize indexing or storing.  相似文献   
8.
The chemical modification of rice flour by phosphorylation is an alternative to improve the technological quality of bakery products. The aim of this study was to investigate the effect of phosphorylation process of rice flour on technological properties (specific volume, crumb and crust colour) of gluten‐free breads and the hardening of these breads during two storage temperatures (21 °C and ?24 °C). Breads were made with native rice flour, with phosphorylated rice flour and with wheat flour, used as control. The phosphorylation causes significant reduction in the synaeresis of pastes and in retrogradation tendency of rice flours, varying from 258.7 cP (native rice flour) to 122 cP (phosphorylated rice flour). The breads prepared with phosphorylated rice flour showed reduction in the hardness in both storage temperatures studied and effect on rice bread volume, crumb appearance and colour, demonstrating the possibility of use of the phosphorylated rice flour in gluten‐free breads.  相似文献   
9.
Power-to-Substitute Natural Gas processes are investigated to offer solutions for renewable energy storing or transportation. In the present study, an original Power-to-SNG process combining high-temperature steam electrolysis and CO2 methanation is implemented and simulated. A reference process is firstly defined, including a specific modelling approach of the electrolysis and a methanation modelling including a kinetic law. The process also integrates a unit to clean the gas from residual CO2, H2 and H2O for gas network injection. Having set all the units, simulations are performed with ProsimPlus 3™ software for a reference case where the electrolyser and the methanation reactors are designed. The reference case allows to produce 67.5 Nm3/h of SNG with an electrical energy consumption of 14.4 kW h/Nm3. The produced SNG satisfies specifications required for network injection. From this reference process, two sensitivity analyses on electrolysis and methanation working points and on external parameters and constraints are considered. As a main result, we observe that the reference case maximises both process efficiency and SNG production when compared with other studied cases.  相似文献   
10.
SPETA: Social pervasive e-Tourism advisor   总被引:1,自引:0,他引:1  
Tourism is one of the major sources of income for many countries. Therefore, providing efficient, real-time service for tourists is a crucial competitive asset which needs to be enhanced using major technological advances. The current research has the objective of integrating technological innovation into an information system, in order to build a better user experience for the tourist. The principal strength of the approach is the fusion of context-aware pervasive systems, GIS systems, social networks and semantics. This paper presents the SPETA system, which uses knowledge of the user’s current location, preferences, as well as a history of past locations, in order to provide the type of recommender services that tourists expect from a real tour guide.  相似文献   
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