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Каталог книг и продолжающихся изданий
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Труды сотрудников Института горного дела УрО РАН
Труды сотрудников Института органического синтеза УрО РАН
Труды сотрудников Института теплофизики УрО РАН
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Труды сотрудников ЦНБ УрО РАН
Публикации Черешнева В.А.
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Каталог библиотеки ИЭРиЖ УрО РАН
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1.
Инвентарный номер: нет.
   
   P 58

   
    Photophysics, photochemistry and bioimaging application of 8-azapurine derivatives / A. K. Eltyshev, I. A. Agafonova, A. S. Minin [et al.] // Organic & biomolecular chemistry. - 2021. - Vol. 19, № 45. - P9880-9896
ББК Г
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: New 2-aryl-1,2,3-triazolopyrimidines were designed, synthesized, and characterized. Their optical properties were thoroughly studied in the solid phase, in solution and in a biological environment. Density Functional Theory (DFT) based calculations were performed, including the molecular geometry optimization for both the ground state and the first singlet excited state, the prediction of the UV-Vis absorption and fluorescence spectra, the determination of the molecular electrostatic properties and the solvent effect on the optical properties. The emission intensity was revealed to increase in time upon irradiation. Mass spectrometric research, quantum mechanical calculations, and analysis of literature data suggested a possible photo-transformation pathway through the homolytic cleavage of one of the C–Cl bonds upon irradiation with UV light. The structure of the active intermediate was identified by the series of mass spectrometry experiments and via synthesis of putative transformation products. The kinetic parameters measured in different solvents allowed estimating the rate of these photo-transformations. Biological experiments demonstrated that 2-aryl-1,2,3-triazolopyrimidines penetrate cells and selectively accumulate in the cell membrane and the Golgi complex and endoplasmic reticulum. Their unique properties pave the way for new possible applications of fluorescent 8-azapurines in biology and medicine.

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2.
Инвентарный номер: нет.
   

   
    Synthesis, characterization, and in vitro assessment of cytotoxicity for novel azaheterocyclic nido-carboranes – Candidates in agents for boron neutron capture therapy (BNCT) of cancer / M. V. Varaksin, L. A. Smyshliaeva, V. L. Rusinov [et al.] // Tetrahedron. - 2021. - Vol. 102. - P132525
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
AZAHETEROCYCLES -- BNCT -- CYTOTOXICITY -- CARBORANES
Аннотация: A series of novel water-soluble azaheterocyclic derivatives of nido-carborane bearing quinoxaline, 2H-imidazole or 1,2,4-triazine moieties were first synthesized in 82–91% yields. The structures of these boron-enriched compounds were confirmed by the data of NMR, IR spectroscopy, and mass spectrometry. To access the toxicity level for these organoboron compounds, the cytotoxicity indexes (IC50) were determined using by the MTT test on both human glioblastoma cell A-172 (IC50 = 150–243 μM) and human embryonic lung cells (IC50 = 424–944 μM) lines. The obtained preliminary results from in vitro analysis enable the synthesized water-soluble azaheterocyclic carboranes to be considered as challenging candidates in the design of agents for boron-neutron capture therapy (BNCT) of malignant tumors.

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3.
Инвентарный номер: нет.
   

   
    Synthesis of mycostatics based on 4-aryldiazenyl-3,5-dimethylpyrazoles / O. G. Khudina, A. E. Ivanova, Ya. V. Burgart [et al.] // Russian chemical bulletin. - 2021. - Vol. 70, № 6. - P1124-1130
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
3-ARYLHYDRAZINYLIDENEPENTANE-2,4-DIONE -- CONDENSATION -- HYDRAZINES -- 4-ARYLDIAZENYL-3,5-DIMETHYLPYRAZOLES
Аннотация: The condensation of 3-arylhydrazinylidenepentane-2,4-diones with hydrazine hydrate, 2-hydroxyethylhydrazine, benzylhydrazine hydrochloride, and 4-hydrazinylbenzenesulfonamide hydrochloride gave 4-aryldiazenyl-3,5-dimethylpyrazoles. An alternative route to the synthesis of N-substituted 4-aryldiazenylpyrazoles is based on the alkylation of NH-pyrazoles with haloalkanes. The synthesized compounds were tested for antimicrobial activity against eight pathogenic dermatophytes, yeast-like fungi of the Candida genus and the bacteria Neisseria gonorrhoeae. The structure—activity relationship analysis showed that 4-tolyldiazenylpyrazoles bearing H, AcO(CH2)4, or HO(CH2)4 substituents at the N(1) atom have the highest mycostatic activity against all the dermatophyte strains under study. However, 4-aryldiazenyl-3,5-dimethylpyrazoles proved to be quite cytotoxic against the McCoy B cell line.

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4.
Инвентарный номер: нет.
   
   U 61

   
    Unsymmetrical trifluoromethyl methoxyphenyl β-diketones: effect of the position of methoxy group and coordination at Cu(II) on biological activity / L. A. Khamidullina, I. S. Puzyrev, P. A. Slepukhin [et al.] // Molecules. - 2021. - Vol. 26, № 21. - Ст. 6466
ББК Г
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
COPPER(II) -- DIKETONATES -- CYTOTOXIC ACTIVITY -- ANTIMICROBIAL ACTIVITY
Аннотация: Copper(II) complexes with 1,1,1-trifluoro-4-(4-methoxyphenyl)butan-2,4-dione (HL1) were synthesized and characterized by elemental analysis, FT-IR spectroscopy, and single crystal X-ray diffraction. The biological properties of HL1 and cis-[Cu(L1)2(DMSO)] (3) were examined against Gram-positive and Gram-negative bacteria and opportunistic unicellular fungi. The cytotoxicity was estimated towards the HeLa and Vero cell lines. Complex 3 demonstrated antibacterial activity towards S. aureus comparable to that of streptomycin, lower antifungal activity than the ligand HL1 and moderate cytotoxicity. The bioactivity was compared with the activity of compounds of similar structures. The effect of changing the position of the methoxy group at the aromatic ring in the ligand moiety of the complexes on their antimicrobial and cytotoxic activity was explored. We propose that complex 3 has lower bioavailability and reduced bioactivity than expected due to strong intermolecular contacts. In addition, molecular docking studies provided theoretical information on the interactions of tested compounds with ribonucleotide reductase subunit R2, as well as the chaperones Hsp70 and Hsp90, which are important biomolecular targets for antitumor and antimicrobial drug search and design. The obtained results revealed that the complexes displayed enhanced affinity over organic ligands. Taken together, the copper(II) complexes with the trifluoromethyl methoxyphenyl-substituted β-diketones could be considered as promising anticancer agents with antibacterial properties

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5.
Инвентарный номер: нет.
   

   
    Boron(III) Complexes with N,​N'- and N,​O-​Heterocyclic Ligands: Synthesis and Spectroscopic Properties [Electronic resource] / G. N. Lipunova, E. V. Nosova, V. N. Charushin, O. N. Chupakhin // Comments on Inorganic Chemistry. - 2016. - Vol. 2016. - С. 1153470
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
PROPERTIES -- PREPARATION -- SYNTHETIC PREPARATION
Аннотация: This review is focused on consideration of effects of the nature of N,​N'- and N,​O-​bidentate ligands on the structure and optical properties of their B(III) complexes. It has been established that B(III) complexes with asym. N,​N'- and N,​O-​bidentate ligands, such as ortho-​hydroxyphenyl substituted azaheterocycles and heteryl-​β-​ketoimines, exhibit large Stokes shifts, enhanced intensity, and extended range for luminescence in solns. as well as in solid state, comparable with characteristics of the family of BODIPYs derivs. Complexes of some bidentate ligands can be considered as promising fluorophores for applications in biomedical imaging, electroluminescent, solar cell devices, and other fields.

\\\\expert2\\nbo\\Comments on Inorganic Chemistry\\2016. P. 1153470.pdf
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6.
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   C 51

   
    Chemoenzymatic Synthesis and Antiherpes Activity of 5-Substituted 4,6-Difluorobenzimidazoles Ribo- and 2′-Deoxyribonucleosides [Электронный ресурс] / M. I. Kharitonova, I. V. Fateev, A. L. Kayushin, I. D. Konstantinova, S. K. Kotovskaya, V. L. Andropova, G. A. Galegov, V. N. Charushin, A. I. Miroshnikov // Synthesis (Germany). - 2016. - Vol. 48, № 3. - С. 394-406. - Bibliogr. : p. 405-406 (37 ref.)
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
DRUG DISCOVERY- -- NUCLEOSIDES -- HERPES SIMPLEX VIRUS
Аннотация: A series of 5,6-disubstituted benzimidazole nucleosides, obtained earlier, did not show any significant antiviral activity at relatively low cytotoxicity in vitro. In the course of our research we have succeeded in introducing an additional fluorine atom into the benzimidazole ring system. A new series of 4,6-difluorobenzimidazoles, bearing various groups (fluoro-, methoxy-, ethoxy-, morpholino-, and pyrrolidino-) in the 5-position of the benzene ring, have been synthesized. All these compounds proved to be substrates for recombinant E. coli purine nucleoside phosphorylase (PNP) in the transglycosylation reaction. Effective methods for the synthesis of ribo- and 2′-deoxyribonucleosides with high yields (60–90%) have been described, and the formation of regioisomeric N3-nucleosides of benzimidazoles have been detected. The biological activity of the nucleosides obtained against herpes simplex virus type 1 (HSV-1) has been elucidated. All compounds show a low cytotoxicity in the cell culture Vero E6. 4,5,6-Trifluoro-1-(β-d-ribofuranosyl)benzimidazole and 5-methoxy-4,6-difluoro-1-(β-d-2′-deoxyribofuranosyl)benzimidazole proved to inhibit completely the progression of the virus cytopathic effect (CPE) at a multiplicity of infection (MOI) of 0.01 PFU/cell.

\\\\expert2\\nbo\\Synthesis\\2016, v. 48. p.394-406.pdf
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7.
Инвентарный номер: нет.
   

   
    Pyrrolylquinoxaline-2-one derivative as a potent therapeutic factor for brain trauma rehabilitation / E. A. Dutysheva, M. A. Mikeladze, N. D. Aksenov [и др.] // Pharmaceutics. - 2020. - Vol. 12, № 5. - С. 414
Кл.слова (ненормированные):
APOPTOSIS -- CEREBROSPINAL FLUID -- HSP70 -- SMALL MOLECULE -- TRAUMATIC BRAIN INJURY
Аннотация: Traumatic brain injury (TBI) often causes massive brain cell death accompanied by the accumulation of toxic factors in interstitial and cerebrospinal fluids. The persistence of the damaged brain area is not transient and may occur within days and weeks. Chaperone Hsp70 is known for its cytoprotective and antiapoptotic activity, and thus, a therapeutic approach based on chemically induced Hsp70 expression may become a promising approach to lower post-traumatic complications. To simulate the processes of secondary damage, we used an animal model of TBI and a cell model based on the cultivation of target cells in the presence of cerebrospinal fluid (CSF) from injured rats. Here we present a novel low molecular weight substance, PQ-29, which induces the synthesis of Hsp70 and empowers the resistance of rat C6 glioma cells to the cytotoxic effect of rat cerebrospinal fluid taken from rats subjected to TBI. In an animal model of TBI, PQ-29 elevated the Hsp70 level in brain cells and significantly slowed the process of the apoptosis in acceptor cells in response to cerebrospinal fluid action. The compound was also shown to rescue the motor function of traumatized rats, thus proving its potential application in rehabilitation therapy after TBI.

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8.
Инвентарный номер: нет.
   
   E 27

   
    Effects of a compound from the group of substituted thiadiazines with hypothermia inducing properties on brain metabolism in rats, a study in vivo and in vitro / O. B. Shevelev, N. B. ILLARIONOVA, D. V. Petrovski, A. P. Sarapultsev, O. N. Chupakhin, M. P. Moshkin // PLOS ONE . - 2017. - Vol. 12, № 7. - С. е0180739[1-12]
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
ГИПОТЕРМИЯ -- HYPOTHERMIA -- 1,3,4-THIADIAZINE -- МЕТАБОЛИТЫ МОЗГА -- BRAIN METABOLITES -- ТЕРМОРЕГУЛЯЦИЯ -- THERMOREGULATION
Аннотация: The aim of the present study was to examine how administration of a compound of 1,3,4-thiadiazine class 2-morpholino-5-phenyl-6H-1,3,4-thiadiazine, hydrobromide (L-17) with hypothermia inducing properties affects the brain metabolism. The mechanism by which L-17 induces hypothermia is unknown; it may involve hypothalamic central thermoregulation as well as act via inhibition of energy metabolism. We tested the hypothesis that L-17 may induce hypothermia by directly inhibiting energy metabolism. The study in vivo was carried out on Sprague-Dawley adult rats. Two doses of L-17 were administered (190 mg/ kg and 760 mg/kg). Brain metabolites were analyzed in control and treated groups using magnetic resonance spectroscopy, along with blood flow rate measurements in carotid arteries and body temperature measurements. Further in vitro studies on primary cultures from rat hippocampus were carried out to perform a mitochondria function test of L-17 preincubation (100 μM, 30 min). Analysis of brain metabolites showed no significant changes in 190 mg/kg treated group along with a significant reduction in body temperature by 1.5ÊC. However, administration of L-17 in higher dose 760 mg/kg provoked changes in brain metabolites indicative of neurotoxicity as well as reduction in carotid arteries flow rate. In addition, a balance change of excitatory and inhibitory neurotransmitters was observed. The L-17 pre-incubation with cell primary cultures from rat brain showed no significant changes in mitochondrial function. The results obtained in the study indicate that acute administration of L-17 190 mg/kg in rats induces mild hypothermia with no adverse effects onto brain metabolism.

\\\\Expert2\\NBO\\PLoS ONE\\2017 V. 12 N 7 p. e0180739.pdf
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9.
Инвентарный номер: нет.
   

   
    Modification of chemically and physically obtained Fe3O4 magnetic nanoparticles with L-Lys for cell labeling / A. M. Demin, O. F. Kandarakov, A. S. Minin [et al.] // Russian chemical bulletin. - 2021. - Vol. 70, № 6. - P1199-1208
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: Peculiar features of the modification of Fe3O4 magnetic nanoparticles (MNPs) obtained by co-precipitation from solutions of FeII and FeIII salts (10-nm MNPs) and by the gas-condensation method (30-nm MNPs) with 3-aminopropylsilane and then with L-lysine were studied. The chemically obtained MNPs possess more pronounced hydrophilic properties and therefore readily form stable aqueous colloidal solutions and can be loaded with a larger amount of L-Lys. However, samples based on the physically obtained MNPs were characterized by more efficient internalization and longer retention times by the NIH 3T3 cells. The results obtained can be used in the design of novel nanomaterials for magnetic cell labeling.

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10.
Инвентарный номер: нет.
   

   
    Stimuli-responsive dual cross-linked N-carboxyethylchitosan hydrogels with tunable dissolution rate / S. Bratskaya, A. Skatova, Y. Privar [et al.] // Gels. - 2021. - Vol. 7, № 4. - Ст. 188
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
HYDROGELS -- CHITOSAN -- SALICYLALDEHYDE
Аннотация: Here, we discuss the applicability of (methylenebis(salicylaldehyde)—MbSA) for the fabrication of the stimuli-responsive N-carboxyethylchitosan (CEC) hydrogels with a tunable dissolution rate under physiological conditions. In comparison with non-covalent salicylimine hydrogels, MbSA cross-linking via covalent bis(‘imine clip’) and non-covalent hydrophobic interactions allowed the fabrication of hydrogels with storage moduli > 1 kPa at ten-fold lower aldehyde/CEC molar ratio with the preservation of pH- and amino-acid responsive behavior. Although MbSA-cross-linked CEC hydrogels were stable at neutral and weakly alkaline pH, their disassembly in cell growth medium (Dulbecco’s modified Eagle’s medium, DMEM) under physiological conditions was feasible due to transimination reaction with amino acids contained in DMEM. Depending on the cross-linking density, the complete dissolution time of the fabricated hydrogels varied from 28 h to 11 days. The cytotoxicity of MbSA cross-linked CEC hydrogels toward a human colon carcinoma cell line (HCT 116) and primary human dermal fibroblasts (HDF) was remarkably lower in comparison with CEC-salicylimine hydrogels. Fast gelation, relatively low cytotoxicity, and tunable stimuli-induced disassembly under physiological conditions make MbSA cross-linked CEC hydrogels promising for drug encapsulation and release, 3D printing, cell culturing, and other biomedical applications.

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