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1.
Sci Rep ; 12(1): 5506, 2022 04 01.
Artigo em Inglês | MEDLINE | ID: mdl-35365721

RESUMO

This article addresses an approach to intelligent safety control of passengers on escalators. The aim is to improve the accuracy of detecting threatening situations on escalators in the subway to make decisions to prevent threats and eliminate the consequences. The novelty of the approach lies in the complex processing of information from three types of sources (video, audio, sensors) using machine learning methods and recurrent neural networks with controlled elements. The conditions and indicators of safety assurance efficiency are clarified. New methods and algorithms for managing the safety of passengers on escalators are proposed. The architecture of a promising safety software system is developed, and implementation of its components for cloud and fog computing environments is provided. Modeling results confirm the capabilities and advantages of the proposed technological solutions for enhancing the safety of escalator passengers, efficiency of control decision making, and system usability. Due to the proposed solutions, it has become possible to increase the speed of identifying situations 3.5 times and increase the accuracy of their determination by 26%. The efficiency of decision making has increased by almost 30%.


Assuntos
Elevadores e Escadas Rolantes , Redes Neurais de Computação , Algoritmos , Gestão da Segurança , Software
2.
Anticancer Agents Med Chem ; 21(5): 597-610, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-32459611

RESUMO

AIMS: The main goal of this work is to synthesize new original spirocyclic hydroxamic acids, investigate their cytotoxicity against the panel of tumor cell lines and possible mechanism of action of these active compounds. BACKGROUND: Hydroxamic acids are one of the promising classes of chemical compounds with proven potential anticancer properties. This is manifested in the presence of metal chelating and antioxidant activities, the ability to inhibit histone deacetylase enzymes and a chemosensitizing effect against well known cytostatics. OBJECTIVE: Original spirocyclic hydroxamic acids were synthesized and spectra of their antiproliferative activities were investigated. METHODS: The cytotoxic activities on different tumor lines (SH-SY5Y, HeLa and healthy cells HEK-293) were investigated and determined possible underlying mechanisms of their activity. RESULTS: New original spirocyclic hydroxamic acids were synthesized. These compounds exhibit antiproliferative properties against various tumor cultures cells and also exhibit antioxidant activity, a depolarizing effect on the mitochondrial membrane, inhibit the activity of the histone deacetylase enzyme, and also decrease of basal glycolysis and glycolytic capacity reserve of HeLa and SH-SY5Y tumor cell lines. CONCLUSION: The most promising are compounds 5j-l containing two chlorine atoms as substituents in the quinazoline part of the molecule and hydroxamate function. Therefore, these compounds can be considered as hit compounds for the development on their basis multi-target anticancer agents.


Assuntos
Antineoplásicos/farmacologia , Ácidos Hidroxâmicos/farmacologia , Compostos de Espiro/farmacologia , Animais , Antineoplásicos/síntese química , Antineoplásicos/química , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Ácidos Hidroxâmicos/síntese química , Ácidos Hidroxâmicos/química , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Estrutura Molecular , Neoplasias Experimentais/tratamento farmacológico , Neoplasias Experimentais/metabolismo , Neoplasias Experimentais/patologia , Ratos , Compostos de Espiro/síntese química , Compostos de Espiro/química , Relação Estrutura-Atividade
3.
J Labelled Comp Radiopharm ; 62(11): 718-728, 2019 09.
Artigo em Inglês | MEDLINE | ID: mdl-31410877

RESUMO

This study aims at analyzing complexation properties of two new short somatostatin analogues, their synthesis, radiolabeling with 44 Sc, 207 Bi, and 152 Eu and stability in vitro. Short tetrapeptide Phe-d-Trp-Lys-Thr and pentapeptide Thz-Phe-d-Trp-Lys-Thr were first conjugated with the DOTA macrocyclic chelator. These conjugates were radiolabeled with 44 Sc, 207 Bi, and 152 Eu and characterized by thin-layer chromatography (TLC) and HPLC. The radiochemical purity was measured using digital autoradiography and gamma spectrometry. Optimum conditions of DOTA-conjugate labeling were found: 0.1mM, pH 8.0 to 8.4 at 90°C for DOTA-tetrapeptide complexes with 207 Bi and 152 Eu; 0.05mM, pH 4.0 to 5.0 at 90°C for 44 Sc-DOTA-tetrapeptide; 0.2mM, pH 4.0 to 5.0 at 90°C for 44 Sc-DOTA-pentapeptide. Complexes of DOTA-pentapeptide with 207 Bi and 152 Eu of radiochemical purity more than 95% were probably unstable at temperature higher than 37°C and were obtained at 37°C, pH 8.0 to 8.4 within 4 days. Mass spectra of the Eu-DOTA-pentapeptide revealed the presence of small fragments of the pentapeptide conjugate in the complex solution. in vitro stability studies were performed in saline in the presence of serum proteins and biologically relevant metal cations. All complexes demonstrated no cation release in vitro within 1 to 4 hours.


Assuntos
Octreotida/química , Octreotida/síntese química , Sequência de Aminoácidos , Animais , Estabilidade de Medicamentos , Compostos Heterocíclicos com 1 Anel/química , Marcação por Isótopo , Tomografia por Emissão de Pósitrons , Radioquímica , Compostos Radiofarmacêuticos/síntese química , Compostos Radiofarmacêuticos/química
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