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Wyniki wyszukiwania dla: ANTICANCER%20AGENTS
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Anticancer imidazoacridinone C-1311 inhibits hypoxia-inducible factor-1α (HIF-1α), vascular endothelial growth factor (VEGF) and angiogenesis
PublikacjaAntitumor imidazoacridinone C-1311 is a DNA-reactive topoisomerase II and FLT3 receptor tyrosine kinase inhibitor. Here, we demonstrate the mechanism of C-1311 inhibitory action on novel targets: hypoxia-inducible factor-1α (HIF-1α), vascular-endothelial growth factor (VEGF), and angiogenesis. In a cell-free system, C-1311 prevented HIF-1α binding to an oligonucleotide encompassing a canonical hypoxia-responsive element (HRE),...
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Synthesis, Molecular Structure, Anticancer Activity, and QSAR Study of N-(aryl/heteroaryl)-4-(1H-pyrrol-1-yl)Benzenesulfonamide Derivatives
PublikacjaA series of N-(aryl/heteroaryl)-4-(1H-pyrrol-1-yl)benzenesulfonamides were synthesized from 4-amino-N-(aryl/heteroaryl)benzenesulfonamides and 2,5-dimethoxytetrahydrofuran. All the synthesized compounds were evaluated for their anticancer activity on HeLa, HCT-116, and MCF-7 human tumor cell lines. Compound 28, bearing 8-quinolinyl moiety, exhibited the most potent anticancer activity against the HCT-116, MCF-7, and HeLa cell lines,...
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Copper(II) Complexes with 1-(Isoquinolin-3-yl)heteroalkyl-2-ones: Synthesis, Structure and Evaluation of Anticancer, Antimicrobial and Antioxidant Potential
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Silylation of acetaminophen by trifluoroacetamide-based silylation agents
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Inhibitors of amino acids biosynthesis as antifungal agents
PublikacjaFungal microorganisms, including the human pathogenic yeast and filamentous fungi, are able to synthesize all proteinogenic amino acids, including nine that are essential for humans. A number of enzymes catalyzing particular steps of human-essential amino acid biosynthesis are fungi specific. Numerous studies have shown that auxotrophic mutants of human pathogenic fungi impaired in biosynthesis of particular amino acids exhibit...
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Essential oils as potential anti-staphylococcal agents
PublikacjaAntibiotic therapy of staphylococcal mastitis is characterized by significantly lower cure rates compared to infections caused by other microorganisms. Thus, it is necessary to search for new, alternative, non-antibiotic agents that are effective in the eradication of these bacteria. The aim of our research was to investigate the antimicrobial, especially anti-staphylococcal potential of a large collection (n=36) of essential oils...
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Decontaminating Arbitrary Graphs by Mobile Agents: a Survey
PublikacjaA team of mobile agents starting from homebases need to visit and clean all nodes of the network. The goal is to find a strategy, which would be optimal in the sense of the number of needed entities, the number of moves performed by them or the completion time of the strategy. Currently, the field of distributed graph searching by a team of mobile agents is rapidly expanding and many new approaches and models are being presented...
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Amino Acid and Peptide‐Based Antiviral Agents
PublikacjaA significant number of antiviral agents used in clinical practice are amino acids, short peptides, or peptidomimetics. Among them, several HIV protease inhibitors (e. g. lopinavir, atazanavir), HCV protease inhibitors (e. g. grazoprevir, glecaprevir), and HCV NS5A protein inhibitors have contributed to a significant decrease in mortality from AIDS and hepatitis. However, there is an ongoing need for the discovery of new antiviral...
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Intercalation complex of imidazoacridinone C-1311, a potential anticancer drug, with DNA helix d(CGATCG)2: stereostructural studies by 2D NMR spectroscopy.
PublikacjaImidazoacridinone C-1311 (Symadex®) is a powerful antitumor agent, which successfully made its way through the Phase I clinical trials and has been recommended for Phase II few a years ago. It has been shown experimentally that during the initial stage of its action C-1311 forms a relatively stable intercalation complex with DNA, yet it has shown no base-sequence specificity while binding to DNA. In this paper, the d(CGATCG)2:C-1311...
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Study of Bioreductive Anticancer Agent RH-1-Induced Signals Leading the Wild-Type p53-Bearing Lung Cancer A549 Cells to Apoptosis
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Novel 2-alkythio-4-chloro-N-[imino(heteroaryl)methyl]benzenesulfonamide Derivatives: Synthesis, Molecular Structure, Anticancer Activity and Metabolic Stability
PublikacjaA series of novel 2-alkythio-4-chloro-N-[imino-(heteroaryl)methyl]benzenesulfonamide derivatives, 8–24, were synthesized in the reaction of the N-(benzenesulfonyl)cyanamide potassium salts 1–7 with the appropriate mercaptoheterocycles. All the synthesized compounds were evaluated for their anticancer activity in HeLa, HCT-116 and MCF-7 cell lines. The most promising compounds, 11–13, molecular hybrids containing benzenesulfonamide...
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Anticancer and antimicrobial properties of novel η6-p-cymene ruthenium(ii) complexes containing a N,S-type ligand, their structural and theoretical characterization
PublikacjaRuthenium(II) complexes are lately of great scientific interest due to their chemotherapeutic potential asanticancer and antimicrobial agents. Here we present the synthesis of new pyrazole carbothioamidederivatives and their four arene–ruthenium complexes. The title compounds were characterized with theapplication of IR, NMR, mass spectrometry, elemental analysis and X-ray diffraction. Additionally, for newcomplexes DFT calculations...
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The Product of Matrix Metalloproteinase Cleavage of Doxorubicin Conjugate for Anticancer Drug Delivery: Calorimetric, Spectroscopic, and Molecular Dynamics Studies on Peptide–Doxorubicin Binding to DNA
PublikacjaMatrix metalloproteinases (MMPs) are extracellular matrix degradation factors, promoting cancer progression. Hence, they could provide an enzyme-assisted delivery of doxorubicin (DOX) in cancer treatment. In the current study, the intercalation process of DOX and tetrapeptide-DOX, the product of the MMPs' cleavage of carrier-linked DOX, into dsDNA was investigated using stationary and time-resolved fluorescence spectroscopy, UV-Vis...
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Control of mass concentration of reagents by sound in a gas with nonequilibrium chemical reactions
PublikacjaThe weakly nonlinear dynamics of a chemically reacting gas is studied. Nonlinear interaction of acoustic and nonacoustic types of motion are considered. We decompose the base equations using the relationships of the gas-dynamic perturbations specific for every type of motion. The governing equation for the mass fraction of a reagent influenced by dominating sound is derived and discussed. The conclusions concern the equilibrium...
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DNA-reactive anticancer imidazoacridinone C-1311 is a new inhibitor of hypoxia-inducible factor 1 alpha, vascular endothelial growth factor and tumor angiogenesis
PublikacjaHypoxia-inducible factor 1 (HIF-1) plays a critical role for tumor adaptation to hypoxia and promotes angiogenesis. Antitumor imidazoacridinone C-1311 is a DNA reactive topoisomerase II and FLT3 receptor tyrosine kinase inhibitor selected for phase II clinical trials for breast cancer. Here, we demonstrate the new mechanism of C-1311 action involving HIF-1a, vascular endothelial growth factor (VEGF) and angiogenesis as additional...
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Bioprocess optimization using response surface methodology for production of the anticancer drug paclitaxel by Aspergillus fumigatus and Alternaria tenuissima: Enhanced production by ultraviolet and gamma irradiation
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AUTONOMOUS AGENTS AND MULTI-AGENT SYSTEMS
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World Research Journal of Antimicrobial Agents
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Cardiovascular and Hematological Agents in Medicinal Chemistry
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Rendezvous of Heterogeneous Mobile Agents in Edge-Weighted Networks
PublikacjaWe introduce a variant of the deterministic rendezvous problem for a pair of heterogeneous agents operating in an undirected graph, which differ in the time they require to traverse particular edges of the graph. Each agent knows the complete topology of the graph and the initial positions of both agents. The agent also knows its own traversal times for all of the edges of the graph, but is unaware of the corresponding traversal...
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Arsenic-Based Warfare Agents: Production, Use, and Destruction
PublikacjaSince the beginning of time, civilizations have looked for more creative ways to dominate and defeat their enemies. The rapid development of the chemical industry just before the Second World War started the era of modern chemical weapon production based on poisons, including toxic arsenic compounds. This paper provides a detailed overview of the production, usage and destruction of this dangerous chemical weapon. Milestones include:...
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Rendezvous of Distance-Aware Mobile Agents in Unknown Graphs
PublikacjaWe study the problem of rendezvous of two mobile agents starting at distinct locations in an unknown graph. The agents have distinct labels and walk in synchronous steps. However the graph is unlabelled and the agents have no means of marking the nodes of the graph and cannot communicate with or see each other until they meet at a node. When the graph is very large we want the time to rendezvous to be independent of the graph size...
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Leader election for anonymous asynchronous agents in arbitrary networks
PublikacjaWe consider the problem of leader election among mobile agents operating in an arbitrary network modeled as an undirected graph. Nodes of the network are unlabeled and all agents are identical. Hence the only way to elect a leader among agents is by exploiting asymmetries in their initial positions in the graph. Agents do not know the graph or their positions in it, hence they must gain this knowledge by navigating in the graph...
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Agents in Simulation of Cyberattacks to Evaluate Security of Critical Infrastructures
PublikacjaIn the last years critical infrastructures have become highly dependent on the information technologies and exposed to cyberattacks. Because the effects of the attacks can be detrimental, it is crucial to comprehensively asses the security of the infrastructures' information systems. This chapter describes MAlSim - the simulator of malicious software based on software agents, developed for the needs of a testbed for critical infrastructures...
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Application of Intelligent Conversational Agents in E-learing Environments
PublikacjaThe paper concerns intelligent tutoring systems and concentrates on apliaction of virtual mentors in distance learning environments. Different educational agent types are described. The prototype of an agent developed at Gdansk University of Technology is also presented, as well as its internal representation and construction. Benefits of virtual mentors applied in distance learning are also pointed out.
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The role and construction of educational agents in distance learning environments
PublikacjaArtykuł przedstawia definicję oraz klasyfikację agentów edukacyjnych. Wskazuje typowe cele i zadania agentów, a także omawia schemat ich budowy i funkcjonowania. Wskazano także różnorodność możliwości, jakie stwarzają różne rodzaje agentów w procesie nauczania. W artykule opisano także wytworzony w ramach badań prototyp agenta WAS, którego zadaniem jest wspomaganie uczniów w zakresie pracy z materiałami edukacyjnymi.
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Rendezvous of heterogeneous mobile agents in edge-weighted networks
PublikacjaWe introduce a variant of the deterministic rendezvous problem for a pair of heterogeneous agents operating in an undirected graph, which differ in the time they require to traverse particular edges of the graph. Each agent knows the complete topology of the graph and the initial positions of both agents. The agent also knows its own traversal times for all of the edges of the graph, but is unaware of the corresponding traversal...
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Synthesis of S-thioacyl dithiophosphates, efficient and chemoselectivethioacylating agents
PublikacjaŁatwo dostępne ditiofosforany acylu izomeryzują do monotiofosforanów O- iS-tioacylu. Reakcja jest odwracalna, więc ogrzewanie ditiofosforanów acylu prowadzi zazwyczaj do powstania mieszaniny izomerycznych bezwodników, która nie może być wykorzystana do wydajnego tioacylowania. Jednak działaniem kwasu ditiofosforowego na mieszaninę izomerycznych bezwodników można wydajnie otrzymać ditiofosforany tioacylu. Związki te to doskonałe...
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Amino Acid Based Antimicrobial Agents – Synthesis and Properties
PublikacjaStructures of several dozen of known antibacterial, antifungal or antiprotozoal agents are based on the amino acid scaffold. In most of them, the amino acid skeleton is of a crucial importance for their antimicrobial activity, since very often they are structural analogs of amino acid intermediates of different microbial biosynthetic pathways. Particularly, some aminophosphonate or aminoboronate analogs of protein amino acids are...
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Gossiping by energy-constrained mobile agents in tree networks
PublikacjaEvery node of an edge-weighted tree network contains a data packet. At some nodes are placed mobile agents, each one possessing an amount of energy (not necessarily the same for all agents). While walking along the network, the agents spend the energy proportionally to the distance traveled and collect copies of the data packets present at the visited network nodes. An agent visiting a node deposits there copies of all currently...
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Mobile chromatographs and spectrometers for the analysis of chemical warfare agents
PublikacjaThis article describes the technological state of readiness regarding mobile chromatographs and spectrometers and their appiicability for the analysis of chemical warfare agents (CWAs), degradation products, simulants, and precursors.
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9,10-Dioxoanthracenyldithiocarbamates effectively inhibit the proliferation of non-small cell lung cancer by targeting multiple protein tyrosine kinases
PublikacjaAnthraquinones have attracted considerable interest in the realm of cancer treatment owing to their potent anticancer properties. This study evaluates the potential of a series of new anthraquinone derivatives as anticancer agents for non-small-cell lung cancer (NSCLC). The compounds were subjected to a range of tests to assess their cytotoxic and apoptotic properties, ability to inhibit colony formation, pro-DNA damage functions,...
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Thermoelectric properties of bismuth-antimony-telluride alloys obtained by reduction of oxide reagents
PublikacjaThe BieSbeTe alloys with different Bi/Sb/Te ratio were fabricated by an innovative method. For that purpose the oxide reagents were melted at high temperature, then quenched to form pellets, milled to a powder and finally reduced in hydrogen at various temperatures. Complex structures consisting of connected thin layers forming a continuous path between nano- and micrometer size grains have been obtained. The electrical conductivity,...
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Regioselective synthesis of novel 4,5-diaryl functionalized 3,4-dihydropyrimidine-2(1H)-thiones via a non-Biginelli-type approach and evaluation of their in vitro anticancer activity
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A novel source of the cardiac glycoside digoxin from the endophytic fungus Epicoccum nigrum : isolation, characterization, production enhancement by gamma irradiation mutagenesis and anticancer activity evaluation
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Therapeutic intervention by the simultaneous inhibition of DNA repair and type I or type II DNA topoisomerases: one strategy, many outcomes
PublikacjaMany anticancer drugs reduce the integrity of DNA, forming strand breaks. This can cause mutations and cancer or cell death if the lesions are not repaired. Interestingly, DNA repair-deficient cancer cells (e.g., those with BRCA1/2 mutations) have been shown to exhibit increased sensitivity to chemotherapy. Based on this observation, a new therapeutic approach termed 'synthetic lethality' has been developed, in which radiation...
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An untraceability protocol for mobile agents and its enhanced security study
PublikacjaArtykuł przedstawia rozszerzoną analizę bezpieczeństwa zaproponowanego przez nas protokołu ochrony przed tropieniem (ang. untraceability protocol) dla agentów mobilnych. Jak dotąd, tak systematyczna analiza bezpieczeństwa nie została przeprowadzona. Co więcej, istniejące znane analizy bezpieczeństwa koncentrują się wyłącznie na atakujących wewnętrznych. Uważamy, że stworzona przez nas lista kontrolna ataków może posłużyć jako...
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Deterministic rendezvous of asynchronous bounded-memory agents in polygonal terrains
PublikacjaWe consider two versions of the rendezvous problem: exact RV, when the points representing agents have to coincide at some time, and e-RV, when these points have to get at distance less than e in the terrain. In any terrain, each agent chooses its trajectory, but the movements of the agent on this trajectory are controlled by an adversary that may, e.g. speed up or slow down the agent.
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Fecal indicators resistance to antimicrobial agents present in municipal wastewater
PublikacjaIn this study removal rate of six antimicrobial compounds (belonging to folate pathway inhibitors and macrolides class) was analyzed in processes of local wastewater treatment plant (WWTP) together with susceptibility patterns of erythromycin (E) resistant Enterococcus spp. and trimethoprim/sulfamethoxazole (SXT) resistant Escherichia coli. According to the obtained data, six of tested antimicrobial agents, namely erythromycin,...
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GROUP COMPOSER - System for Modeling Agents’ Team Building for Tasks
PublikacjaMulti-agent systems consist of many autonomous units, called agents, that can interact when trying to achieve their goals. The selection of interaction partners is called team formation. Three basic approaches can be considered to match multi-agent system resources to the problem at hand. To research the properties of different approaches, a software for modeling team formation in multi-agent systems has been created and is presented...
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Harmful biological agents in municipal waste thermal treatment plants
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Deterministic rendezvous of asynchronous bounded-memory agents in polygonal terrains
PublikacjaTwo mobile agents, modeled as points starting at differentlocations of an unknown terrain, have to meet. The terrain is a polygon with polygonal holes. We consider two versions of this rendezvous problem: exact RV, when the points representing the agents have to coincide at some time, and epsilon-RV, when these points have to get at distance less than epsilon in the terrain. In any terrain, each agent chooses its trajectory, but...
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The Influence of Binding Agents on Stiffness of Mineral-cement-emulsion Mixtures
PublikacjaThis paper attempts to determine the behavior of mineral-cement-emulsion mixture (MCE) under load, whether is it similar to asphalt mixtures (viscoelastic behavior) or to cement treated materials (elastic behavior). To answer this question nine mineral- cement-emulsion mixtures with different combinations of cement and emulsion content were tested in laboratory using Simple Performance Test (SPT). For each mixture stiffness moduli...
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Big Data Processing by Volunteer Computing Supported by Intelligent Agents
PublikacjaIn this paper, volunteer computing systems have been proposed for big data processing. Moreover, intelligent agents have been developed to efficiency improvement of a grid middleware layer. In consequence, an intelligent volunteer grid has been equipped with agents that belong to five sets. The first one consists of some user tasks. Furthermore, two kinds of semi-intelligent tasks have been introduced to implement a middleware...
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The Usefulness of Cyclic Diamidines with Different Core-substituents as Antitumor Agents
PublikacjaA series of related polycationic compds. has been screened for potential antitumor activity by the NCI's in vitro testing (one dose primary anticancer assay and the NCI-60 full panel screening). The GI50 values of triazines 3 and 4 are on av. 1.9 μM and 2.4 μM, resp. Furan 8 deserves mention too (1.9 μM). The biol. test results showed that carbazole 10 possessed cytotoxic activity in the nanomolar range, much better than...
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Quantum strategies for rendezvous and domination tasks on graphs with mobile agents
PublikacjaThis paper explores the application of quantum nonlocality, a renowned and unique phenomenon acknowledged as a valuable resource. Focusing on an alternative application, we demonstrate its quantum advantage for mobile agents engaged in specific distributed tasks without communication. The research addresses the significant challenge of rendezvous on graphs and introduces a distributed task for mobile agents grounded in the graph...
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Concept of the mobile monitoring system for chemical agents control in the air
PublikacjaW artykule przedstawiono koncepcję mobilnego systemu monitoringu związków chemicznych zanieczyszczających powietrze. Nowością w przedstawionej koncepcji monitoringu jest pomiar zanieczyszczeń powietrza wzdłuż ciągów komunikacyjnych, co do tej pory nie jest realizowane. W tym celu przedstawiono propozycję rozwiązania stosunkowo małego, bezobsługowego modułu do pomiarów związków chemicznych, który z łatwością będzie montowany na...
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Selection of derivatisation agents for chlorophenols determination with multicriteria decision analysis
PublikacjaThe paper shows very systematic method of selection of derivatisation agents for a given group of analytes. In this study 8 derivatisation agents are assessed for their capability to derivatise 8 chlorophenols. Multicriteria decision analysis is used to combine many objectives of derivatisation agents selection into single, easy to be interpreted numerical value. Three basic analyses were performed to obtain rankings with the aims...
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Constructing autonomous agents using the cognitive-emotional architecture of the mind
PublikacjaThe article discusses an important issue regarding the humanoid aspects of modern science related to the autonomy of systems and robotization. Particular attention is paid to the basic aspects of cognitive architecture. After a short introduction, the Intelligent Decision Making System, developed at the ETI Faculty of the Gdańsk University of Technology, is described.
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A Review of Traffic Analysis Attacks and Countermeasures in Mobile Agents' Networks
PublikacjaFor traditional, message-based communication, traffic analysis has been already studied for over three decades and during that time various attacks have been recognised. As far as mobile agents’ networks are concerned only a few, specific-scope studies have been conducted. This leaves a gap that needs to be addressed as nowadays, in the era of Big Data, the Internet of Things, Smart Infrastructures and growing concerns for privacy,...