Computer-Aided Search for 5-Arylideneimidazolone Anticancer Agents Able To Overcome ABCB1-Based Multidrug Resistance

ABCB1 modulation is an interesting strategy in the search for new anticancer agents that can overcome multidrug resistance (MDR). Hence, 17 new 5-arylideneimidazolones containing an amine moiety, as potential ABCB1 inhibitors, were designed, synthesized, and investigated. The series was tested in both parental (PAR) and multidrug-resistant (MDR) ABCB1-overexpressing T-lymphoma cancer cells using cytotoxicity assays. The ABCB1-modulating activity was examined in rhodamine 123 accumulation tests, followed by Pgp-Glo™ Assay to determine the influence of the most active compounds on ATPase activity. Lipophilic properties were assessed both, in silico and experimentally (RP-TLC). Pharmacophore-based molecular modelling toward ABCB1 modulation was performed. The studies allowed the identification of anticancer agents (p-fluorobenzylidene derivatives) more potent than doxorubicin, with highly selective action on MDR T-lymphoma cells (selectivity index >40). Most of the investigated compounds showed ABCB1-modulating action; in particular, two 5-benzyloxybenzylidene derivatives displayed activity nearly as strong as that of tariquidar.     

Effect of Ca2+ and Mg2+ ions on the sintering and spectroscopic properties of cr-doped yttrium aluminum garnet ceramics

In this work, we investigated the effects of Ca²⁺ and Mg²⁺ ions and annealing temperature on the spectroscopic parameters of chromium-doped yttrium aluminum garnet ceramics (Cr:YAG). Samples were obtained with either a separate or a simultaneous addition of calcium and magnesium oxides. To achieve this, aqueous suspensions were prepared using Y₂O₃, Al₂O₃, Cr₂O₃, MgO, and CaO high-purity powders as raw materials. The obtained suspensions were freeze-granulated, pressed into pellets, debinded, and subjected to reactive sintering in vacuum at 1715°C for 6 h. Each material was annealed in air with temperatures between 1300 and 1700°C. Samples were also compared to Cr:YAG ceramics with the addition of silica as a sintering aid. All the materials obtained were then exposed to 445 nm excitation, and emission spectra in the visible and infrared wavelengths were recorded. The results showed that the emission spectra of Cr:YAG ceramics varied according to the annealing conditions: as-sintered samples exhibited strong emissions of around 680 nm and, after air annealing, of around 1400 nm. This phenomenon is attributed to the Cr³⁺→Cr⁴⁺ transition. Samples doped solely with MgO exhibited the highest emission intensity in the infrared region. Thus, Mg²⁺ ions provided the best conversion efficiency of chromium ions.     

Stability of nonlinear 2D systems described by the continuous-time Roesser model

This paper considers systems with two-dimensional dynamics (2D systems) described by the continuous-time nonlinear state-space Roesser model. The sufficient conditions of exponential stability in terms of vector Lyapunov functions are established. These conditions are then applied to analysis of the absolute stability of a certain class of systems comprising a linear continuous-time plant in the form of the Roesser model with a nonlinear characteristic in the feedback loop, which satisfies quadratic constraints. The absolute stability conditions are reduced to computable expressions in the form of linear matrix inequalities. The obtained results are extended to the class of continuous-time systems governed by the Roesser model with Markovian switching. The problems of absolute stability and stabilization via state- and output-feedback are solved for linear systems of the above class. The solution procedures for these problems are in the form of algorithms based on linear matrix inequalities.     

Comments on “Necessary and sufficient stability condition of fractional-order interval linear systems” [Automatica 44 (2008), 2985–2988]

This paper shows that the main thesis of the article “Necessary and sufficient stability condition of fractional-order interval linear systems” by Ahn and Chen (Automatica, vol. 44, pp. 2985–2988) is only a sufficient (and not a necessary) condition for the robust stability of fractional-order linear systems.     

Production of nanoparticles of copper compounds by anodic dissolution of copper in organic solvents

The anodic behaviour of copper was investigated in ethanol solution containing LiClO₄, LiCl electrolyte and water. The type of electrolyte and the water content influences the mechanism of the anodic process and the formation of anodic products. In LiClO₄ electrolyte the dissolution of copper is related to the oxidation of Cu(I) to Cu(II). In solutions of LiCl the etching of copper begins with the creation of soluble complexes of Cu(I) with chloride ions and solvent molecules. At potentials above 0.4 V the formation of alkoxides was observed in both solutions, characterized by a yellow tint. On the other hand, above 0.8 V (i.e. above the equilibrium potential of alcohol oxidation) copper dissolution is accompanied by the formation of a blue colloidal suspension of Cu (II) copper salt. Anodic etching of copper in solutions containing 3% H₂O at potentials higher than 0.4 V leads to the formation of colloidal suspension of copper oxide nanoparticles.     

Seed Selection for Spread of Influence in Social Networks: Temporal vs. Static Approach

The problem of finding optimal set of users for influencing others in the social network has been widely studied. Because it is NP-hard, some heuristics were proposed to find sub-optimal solutions. Still, one of the commonly used assumption is the one that seeds are chosen on the static network, not the dynamic one. This static approach is in fact far from the real-world networks, where new nodes may appear and old ones dynamically disappear in course of time. The main purpose of this paper is to analyse how the results of one of the typical models for spread of influence - linear threshold - differ depending on the strategy of building the social network used later for choosing seeds. To show the impact of network creation strategy on the final number of influenced nodes - outcome of spread of influence, the results for three approaches were studied: one static and two temporal with different granularities, i.e. various number of time windows. Social networks for each time window encapsulated dynamic changes in the network structure. Calculation of various node structural measures like degree or betweenness respected these changes by means of forgetting mechanism - more recent data had greater influence on node measure values. These measures were, in turn, used for node ranking and their selection for seeding. All concepts were applied to experimental verification on five real datasets. The results revealed that temporal approach is always better than static and the higher granularity in the temporal social network while seeding, the more finally influenced nodes. Additionally, outdegree measure with exponential forgetting typically outperformed other time-dependent structural measures, if used for seed candidate ranking.     

New method for the on-line signature verification based on horizontal partitioning

Verification of identity based on the analysis of dynamic signatures is an important problem of biometrics. The effectiveness of the verification significantly increases when the dynamic characteristics of signature (e.g. velocity of the pen) are considered. These characteristics are individual for each user and difficult to imitate. The effectiveness of the verification can be further improved by using partitioning. In this paper we propose a new method which uses partitioning. In our method partitions represent areas of high and low speed of signature and high and low pen?s pressure. All selected partitions are used by our algorithm, but more important in the classification process are these partitions, in which the signatures of the user acquired during training phase are more stable. Moreover, final classification is interpretable. In this paper we present the simulation results of the proposed method for the two databases: SVC2004 and BioSecure Database.