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Polygodial, a terpenoid dialdehyde isolated from Polygonum hydropiper L., is a known agonist of the transient receptor potential vanilloid 1 (TRPV1). In this investigation a series of polygodial analogues were prepared and investigated for TRPV1‐agonist and anticancer activities. These experiments led to the identification of 9‐epipolygodial, which has antiproliferative potency significantly exceeding that of polygodial. 9‐Epipolygodial was found to maintain potency against apoptosis‐resistant cancer cells as well as those displaying the multidrug‐resistant (MDR) phenotype. In addition, the chemical feasibility for the previously proposed mechanism of action of polygodial, involving the formation of a Paal–Knorr pyrrole with a lysine residue on the target protein, was demonstrated by the synthesis of a stable polygodial pyrrole derivative. These studies reveal rich chemical and biological properties associated with polygodial and its direct derivatives. These compounds should inspire further work in this area aimed at the development of new pharmacological agents, or the exploration of novel mechanisms of covalent modification of biological molecules with natural products.  相似文献   
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Multimedia Tools and Applications - In recent years, enormous people in all age category were affected with epilepsy throughout the world. To detect and evaluate the epilepsy seizure, the...  相似文献   
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In general,packaging materials which encapsulate light emitting diodes(LEDs)and microelectronic devices offer barrier protection against several environmental hazards such as water and ionic contaminants.However,these encapsulants may provide pathways for water and ionic contaminants to reach the metal/polymer interfaces and provoke local corrosion of electronics,which is a major reliability concern for polymer encapsulated LEDs and microelectronics.As the water and corrosive constituents play a crucial role in their reliability,water uptake kinetics,interfacial ion transport and delamination behaviour of silicone coated copper model system,mimicking a typical microelectronics packaging system,is explored in the present work.Electrochemical impedance spectroscopy(EIS)integrated with attenuated total reflection Fourier transform infrared(ATR-FTIR)spectroscopy studies revealed that water diffusion inside the silicone network is Fickian in nature and the evolution of the observed time constants are related to the diffusion and interfacial reactions.A decrease of impedance magnitude with time was observed in EIS measurements concurrently with water absorption bands shifting towards lower wavenumber in ATR-FTIR measurements,implying the growth of strong hydrogen bonding between water molecules and the silicone network.The estimated diffusion constant of water using the capacitance method was in the order of 7×10-12m2s-1and the water absorption volume fraction was in the range of 0%to 0.30%.Scanning Kelvin probe studies elucidated the ion transport process occurring at the silicone/copper interface in a humid atmosphere.The interfacial ion transport process is controlled by the interfacial electrochemical reactions at the cathodic delamination front and the estimated average delamination rate is 0.43 mm h-1/2.This work demonstrates that exploring ion and water transport in the silicone coating and along the silicone/copper interface is of pivotal importance as part of a detailed reliability assessment of the polymer encapsulated LEDs and microelectronics.  相似文献   
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Preprocessing of data is ubiquitous, and choosing significant attributes has been one of the important steps in the prior processing of data. Feature selection is used to create a subset of relevant feature for effective classification of data. In a classification of high-dimensional data, the classifier usually depends on the feature subset that has been used for classification. The Relief algorithm is a popular heuristic approach to select significant feature subsets. The Relief algorithm estimates feature individually and selects top-scored feature for subset generation. Many extensions of the Relief algorithm have been developed. However, an important defect in the Relief-based algorithms has been ignored for years. Because of the uncertainty and noise of the instances used for measuring the feature score in the Relief algorithm, the outcome results will vacillate with the instances, which lead to poor classification accuracy. To fix this problem, a novel feature selection algorithm based on Chebyshev distance-outlier detection model is proposed called noisy feature removal-Relief, NFR-ReliefF in short. To demonstrate the performance of NFR-ReliefF algorithm, an extensive experiment, including classification tests, has been carried out on nine benchmarking high-dimensional datasets by uniting the proposed model with standard classifiers, including the naïve Bayes, C4.5 and KNN. The results prove that NFR-ReliefF outperforms the other models on most tested datasets.

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Journal of Materials Science - The composite approach is very effective in developing multiferroic systems with remarkable magnetoelectric coupling coefficients. In this work, P(VDF-HFP)-based...  相似文献   
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This review surveys the recent developments to perform heterogeneous catalysis in continuous‐flow microreactors. Three different types, namely, (i) packed‐bed, (ii) monolithic, and (iii) wall‐coated approaches are discussed to implement various kinds of catalysts in a microreactor. In addition, the applications of these supported catalysts to perform a variety of organic reactions are described. Furthermore, advantages of catalytic microreactors over classical batch reactors on one or more aspects of the reaction, such as rate, conversion, selectivity, and enantioselectivity are presented.

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7.
Culex (Culiciomyia) spathifurca (Edwards) is recorded for the 1st time in India. Immature specimens of this species were collected from tree holes in a mangrove forest. Notes on the larval habitat are given.  相似文献   
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