Design, Synthesis, and Antitumor Potential of New Thiazole--contained 5-Fluoro-2-Oxindole Derivatives as Sunitinib Analogues.

Background: Indole is considered the most promising scaffold for anticancer drug design due to its high bioavailability, unique chemical properties, and broad spectrum of pharmacological action.

Objective: Twelve novel thiazole-containing the 5-fluoro-1,3-dihydro-2H-indol-2-one derivatives as sunitinib analogs were designed and synthesized, and their anticancer activity was evaluated against the NCI-60 cancer cell lines.

Method: The thiazole-contained 5-fluoro-1,3-dihydro-2H-indol-2-one derivatives were synthesized using Knoevenagel condensation of 1,3-thiazole-5-carboxylic acid 1.

Synthesis, Characterization, In Vitro Anticancer Evaluation, ADMET Properties, and Molecular Docking of Novel 5-Sulfanyl Substituted (Thiazol-4-yl)-Phosphonium Salts.

Seven TPP+ new 5-sulfanyl substituted (thiazol-4-yl) phosphonium salts functionalized with different substituents were designed, synthesized, and studied against the NCI-60 human cancer cell lines. Compounds 1-4 show the total average parameters GI=0.7-2.

Synthesis, characterization of novel N-(4-cyano-1,3-oxazol-5-yl)sulfonamide derivatives and in vitro screening their activity against NCI-60 cancer cell lines.

A novel series of N-(4-cyano-1,3-oxazol-5-yl)sulfonamides have been synthesized and characterized by IR, H NMR, C NMR spectroscopy, elemental analysis and chromato-mass-spectrometry. The anticancer activities of all newly synthesized compounds were evaluated via a single high-dose assay (10 μM) against 60 cancer cell lines by the National Cancer Institute (USA) according to its screening protocol. Among them, compounds 2 and 10 exhibited the highest activity against the 60 cancer cell lines panel in the one-dose assay.

Synthesis, Characterization and in vitro Anticancer Evaluation of 5-Sulfinyl(sulfonyl)-4-arylsulfonyl-Substituted 1,3-Oxazoles.

A novel series of 5-sulfinyl(sulfonyl)-4-arylsulfonyl-substituted 1,3-oxazoles has been synthesized, characterized and subjected to NCI in vitro assessment. Cancer cell lines of all subpanels were most sensitive to 2-{[4-[(4-fluorophenyl)sulfonyl]-2-(2-furyl)-1,3-oxazol-5-yl]sulfinyl}acetamide (3 l). Its antiproliferative and cytotoxic activity averaged over each subpanel was manifested in a very narrow range of concentrations (GI : 1.

Design, synthesis and evaluation of the anti-breast cancer activity of 1,3-oxazolo[4,5-]pyrimidine and 1,3-oxazolo[5,4-]pyrimidine derivatives.

A series of 1,3-oxazolo[4,5-]pyrimidine and 1,3-oxazolo[5,4-]pyrimidine derivatives were synthesized and functionalized in this study. The obtained compounds were tested against breast cancer cell lines of the NCI subpanel, followed by further analysis using the COMPARE algorithm from the Therapeutics Development Program, NCI. All synthesized derivatives displayed activity against most cell lines in the range of micromolar concentrations in terms of all parameters studied.

Evaluation of Anticancer Activity of 1,3-Oxazol-4-ylphosphonium Salts in Vitro.

A novel series of 1,3-oxazol-4-yltriphenylphosphonium salts has been synthesized and functionalized. Oxazole derivatives were subjected to NCI in vitro assessment. Seven most active derivatives have been selected for five-dose assay.

Genome Features of Probiotic Bifidobacteria Determining Their Strain-Specific Properties.

Unlabelled: was to analyze the genome features of the probiotic strains 379, 1, and 791 and study their antiviral activity.

Materials And Methods: Whole genome sequencing of three strains of bifidobacteria was performed on the MiSeq platform (Illumina Inc., USA).

Colon Microbiocenosis and Its Correction in Patients Receiving Programmed Hemodialysis.

Unlabelled: was to study the species composition of colon microbiocenosis in patients with chronic kidney disease receiving programmed hemodialysis treatment and to evaluate the efficacy of its correction using a new immobilized synbiotic.

Materials And Methods: Samples of colon microbiota from 62 patients undergoing programmed hemodialysis were studied before and after a course of diet therapy that included probiotic components, in particular, the immobilized synbiotic LB-complex L. Isolation of microorganisms was carried out according to our original method; for bacteria identification, a MALDI-TOF Autoflex speed mass spectrometer (Bruker Daltonik, Germany) was used in the Biotyper program mode.

Genome Features and Activity against Influenza A and SARS-CoV-2 Viruses of Six Probiotic Strains.

Purpose: The aim of this work was to analyze the complete genome of probiotic bacteria 8 RA 3, 90 TC-4, 39, 791, 1, and 379 and to test their activity against influenza A and SARS-CoV-2 viruses.

Methods: To confirm the taxonomic affiliation of the bacterial strains, MALDI TOF mass spectrometry and biochemical test systems were used. Whole genome sequencing was performed on the Illumina Inc.

Intrinsic drug potential of oxazolo[5,4-d]pyrimidines and oxazolo[4,5-d]pyrimidines.

The oxazole and pyrimidine rings are widely displayed in natural products and synthetic molecules. They are known as the prime skeletons for drug discovery. On the account of structural and chemical diversity, oxazole and pyrimidine-based molecules, as central scaffolds, not only provide different types of interactions with various receptors and enzymes, showing broad biological activities, but also occupy a core position in medicinal chemistry, showing their importance for development and discovery of newer potential therapeutic agents (Curr Top Med Chem, 16, 2016, 3133; Int J Pharm Pharm Sci, 8, 2016, 8; BMC Chem, 13, 2019, 44).

[Lactobacillus fermentum 90 TC-4 taxonomic status confirmation using whole genome sequencing and MALDI TOF mass spectrum].

With the use of whole genome sequencing, the taxonomic status of Lactobacillus fermentum 90 TC-4 strain from Russian collections were studied. Complex analysis of phenotypical and genetic properties was conducted using phenotypic and molecular genetic methods. The main characteristics of the genome and biochemical activity profile of the strain were determined.

[CHARACTERISTICS OF BIOLOGICAL AND MOLECULAR-GENETIC PROPERTIES OF LACTOBACILLUS FERMENTUM 90 TC-4 PROBIOTIC STRAIN].

Aim: Confirmation of taxonomic position of Lactobacillus fermentum 90 TC-4 strain using phenotypic (classic microbiological, MALDI TOF mass-spectrometry) and genetic (16S rRNA gene segment sequencing and full genome sequencing) methods.

Materials And Methods: Object of the study--Lactobacillus fermentum 90 TC-4 strains from various collections. Mass-spectrometric analysis was carried out using Autoflex MALDI TOF mass-spectrometer (Bruker Daltonics, Germany), study of biochemical properties of the strain was carried out using API 50 CHL strips (Biomerueux, France), "DNA-sorb B" kitwas used for isolation ofgenome DNA (CRIE, Moscow).

Nucleic acid memory.

Nucleic acid memory has a retention time far exceeding electronic memory. As an alternative storage media, DNA surpasses the information density and energy of operation offered by flash memory.

Zeta potential response of human erythrocyte membranes to the modulators of Gardos channel activity under low rate β-radiation.

Objective: Study of human erythrocyte DP response under modification by activators and blockers of the functional state of Ca2+-dependent K+ channels under low rate β-radiation.

Materials And Methods: Erythrocytes were isolated from the donor blood. The zeta potential was computed from the value of the cell electrophoretic mobility.

The osmotic resistance, and zeta potential responses of human erythrocytes to transmembrane modification of Ca2+ fluxes in the presence of the imposed low rate radiation field of 90Sr.

Purpose: To investigate the effects of the imposed low dose rate ionizing field on membrane stability of human erythrocytes under modulation of transmembrane exchange of Ca(2+).

Materials And Methods: Osmotic resistance of human erythrocytes was determined by a measure of haemoglobin released from erythrocytes when placed in a medium containing serial dilutions of Krebs isotonic buffer. The zeta potential as indicator of surface membrane potential was calculated from value of the cellular electrophoretic mobility.

[Participation of proteinkinase CK2 in regulation of human erythrocytes plasma membrane redox system activity: relative contribution of ca(2+)-dependent and ca(2+)-independent mechanisms of its activation].

Involvement of protein kinase CK2 (2.7.11.

Scaling limits of resistive memories.

This paper is intended to provide an expository, physics-based, framework for the estimation of the performance potential and physical scaling limits of resistive memory. The approach taken seeks to provide physical insights into those parameters and physical effects that define device performance and scaling properties. The mechanisms of resistive switching are based on atomic rearrangements in a material.

The effects of ultra-low dose beta-radiation on the physical properties of human erythrocyte membranes.

Purpose: To determine the effects of ultra-low dose beta-radiation (ULDBR) on the physical properties of human erythrocyte membranes.

Materials And Methods: To study the structural changes induced by beta-radiation in erythrocyte ghosts, the interactions of fluorescent probes (1-anilino-8-naphthalene sulfonate, pyrene) with the erythrocyte membranes were investigated. The fluorescent responses to the ULDBR were registered after the addition of (14)C-leucine (37-3700 kBq(l(-1)) in the cellular suspension.

[Sodium azide as indirect nitric oxide donor: researches on the rat aorta isolated segments].

A comparative investigations of heme-containing enzymes inhibitors NaN3 and NaCN effects on the rat aorta isolated segments tone has shown that NaN3 in the range of very low concentrations from 10(-9) to 10(-6) M displays pharmacological activity characteristic of nitric oxide (NO) donors, which is inhibited by NaCN. The value of vasodilatation, caused by NaN3, was also decreased in the presence of soluble guanylate cyclase inhibitor ODQ (10(-5) M). It was found that H2O2 injection to physiological solution containing NaN3 and horseradish peroxidase or catalase lead to NO2- accumulation in it, which was blocked by NaCN.

Ultra-low dose beta-irradiation induces constriction of rabbit carotid arteries via the endothelium.

Purpose: To investigate the action of ultra-low dose beta-radiation (ULDBR) on isolated segments of blood vessels.

Materials And Methods: We used the pharmacological model of isolated rabbit carotid arteries with intact or mechanically removed endothelium. Specific vascular responses to beta-irradiation were registered after addition of (90)Sr in the concentration range between 12 and 96 microCi l(-1) to the organ bath containing physiological salt solution (PSS).

[Influence of beta-radiation on human erythrocyte surface potential under eicosanoid metabolism inhibition].

The aim of the research consisted in the study of influence of beta-radiation on response of erythrocyte surface potential to inhibitors of eicosanoid metabolism enzymes (cyclo-, lipoxygenase and phospholipase A2). It was shown, that inhibitors of phospholipase A2 (quinacrine, 10-100 microM), cyclooxygenase (aspirin, 10-100 microM) and cyclo- and lipoxygenase (BW755c, 1-100 microM) lowered electrophoretic mobility (EPM) of erythrocytes by 20-30%. An analogous effect can be exerted by beta-radiation.