Novel Hybrid Compounds Containing Benzofuroxan and Aminothiazole Scaffolds: Synthesis and Evaluation of Their Anticancer Activity

A series of novel hybrid compounds containing benzofuroxan and 2-aminothiazole moieties are synthesized via aromatic nucleophilic substitution reaction. Possible reaction pathways have been considered quantum-chemically, which allowed us to suggest the most probable products. The quantum chemical results have been proved by X-ray data on one compound belonging to the synthesized series. It was shown that the introduction of substituents to both the thiazole and amine moieties of the compounds under study strongly influences their UV/Vis spectra. Initial substances and obtained hybrid compounds have been tested in vitro as anticancer agents. Target compounds showed selectivity towards M-HeLa tumor cell lines and were found to be more active than starting benzofuroxan and aminothiazoles. Furthermore, they are considerably less toxic to normal liver cells compared to Tamoxifen. The mechanism of action of the studied compounds can be associated with the induction of apoptosis, which proceeds along the mitochondrial pathway. Thus, new hybrids of benzofuroxan are promising candidates for further development as anticancer agents.     

The atomic and electronic structure of oxygen polyvacancies in anatase

We investigate oxygen-deficient anatase using quantum-chemical simulation within the density functional theory and X-ray photoelectron spectroscopy. It is demonstrated that etching of anatase with argon ions with an energy of 2.4 keV results in the formation of oxygen vacancies and polyvacancies at a concentration of approximately 10²⁰ cm^–3 in the crystal. It was found that the most energetically favorable spatial configuration of an oxygen polyvacancy is a three-dimensional chain in crystallographic direction [100] or [010]. The ability of oxygen polyvacancy in the form of a chain to act as a conductive filament and to participate in the resistive switching is discussed.     

Debt Portfolio Management for an Oil Company Under Oil Price Uncertainty

The issue of discovering an optimal debt portfolio in case of oil company under oil price uncertainty is considered in the paper. New algorithm to build optimal debt structure is proposed. It is shown that optimal portfolio reduces financial risk in case of oil price uncertainty. Non-parametric approximation is used to describe functional relationship between US dollar and Russian ruble, considered as commodity currency.     

Production of high-energy fuel with low volatile content from 3B and D coal

Experiments on the carbonization of coal show that high-energy fuel with satisfactory piece strength (??8 MPa in compression) may be produced in the nonoxidative heating of 3B and D coal, with gradual increase in the furnace temperature from 300 to 600°C. Such fuel does not require briquetting.     

Surface Roughness in the Machining of F-4K20 Composite

Russian Engineering Research - The influence of the machining conditions (cutting depth, cutting speed, and supply) on the surface roughness of an F-4K20 composite plate in turning by a cutter...     

Epidural Stimulation Combined with Triple Gene Therapy for Spinal Cord Injury Treatment

The translation of new therapies for spinal cord injury to clinical trials can be facilitated with large animal models close in morpho-physiological scale to humans. Here, we report functional restoration and morphological reorganization after spinal contusion in pigs, following a combined treatment of locomotor training facilitated with epidural electrical stimulation (EES) and cell-mediated triple gene therapy with umbilical cord blood mononuclear cells overexpressing recombinant vascular endothelial growth factor, glial-derived neurotrophic factor, and neural cell adhesion molecule. Preliminary results obtained on a small sample of pigs 2 months after spinal contusion revealed the difference in post-traumatic spinal cord outcomes in control and treated animals. In treated pigs, motor performance was enabled by EES and the corresponding morpho-functional changes in hind limb skeletal muscles were accompanied by the reorganization of the glial cell, the reaction of stress cell, and synaptic proteins. Our data demonstrate effects of combined EES-facilitated motor training and cell-mediated triple gene therapy after spinal contusion in large animals, informing a background for further animal studies and clinical translation.     

Calix[4]arene Polyamine Triazoles: Synthesis,Aggregation and DNA Binding

Artificial gene delivery systems are in great demand from both scientific and practical biomedical points of view. In this paper, we present the synthesis of a new click chemistry calix[4]arene precursor with free lower rim and new water-soluble calixarene triazoles with 12 amino-groups on the upper rim (one with free phenol hydroxyl groups and two another containing four butyl or tetradecyl fragments). Aggregation in the series of amino-triazole calixarenes of different lipophilicity (calixarene with free phenol hydroxyl groups or butyl and tetradecyl fragments on the lower rim) was studied using dynamic light scattering and fluorescent pyrene probe. It was found that calix[4]arene with a free lower rim, like alkyl-substituted butyl calix[4]arene, forms stable submicron aggregates 150–200 nm in size, while the more lipophilic tetradecyl –substituted calix[4]arene forms micellar aggregates19 nm in size. Using UV-Vis spectroscopy, fluorimetry and CD, it was shown that amino-triazole calix[4]arenes bind to calf thymus DNA by classical intercalation. According to DLS and TEM data, all studied macrocycles cause significant DNA compaction, forming stable nanoparticles 50–20 nm in size. Among all studied calix[4]arenes the most lipophilic tetradecyl one proved to be the best for both binding and compaction of DNA.     

A Technique for Measuring Beta-Spectrograms on a МАС-1 Universal Setup

Methods for processing the photographic spectrograms of internal-conversion electrons are considered. The spectograms were obtained on a beta-spectrograph for rare-earth elements isotopes with the use of a precision TV image-reading system designed in 2000 for the MAC-1 setup.