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Каталог книг и продолжающихся изданий
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Труды Института высокотемпературной электрохимии УрО РАН
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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.
Публикации Чарушина В.Н.
Каталог библиотеки ИЭРиЖ УрО РАН
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Общее количество найденных документов : 33
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1.
Инвентарный номер: нет.
   

   
    Variation in tumor pH affects pH-triggered delivery of peptide-modified magnetic nanoparticles / A. G. Pershina, O. Y. Brikunova, S. V. Vtorushin [et al.] // Nanomedicine: nanotechnology, biology and medicine. - 2021. - Vol. 32. - P102317
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
PH PROFILE -- ENDOCYTOSIS -- IRON OXIDE MAGNETIC NANOPARTICLES
Аннотация: Acidification of the extracellular matrix, an intrinsic characteristic of many solid tumors, is widely exploited for physiologically triggered delivery of contrast agents, drugs, and nanoparticles to tumor. However, pH of tumor microenvironment shows intra- and inter-tumor variation. Herein, we investigate the impact of this variation on pH-triggered delivery of magnetic nanoparticles (MNPs) modified with pH-(low)-insertion peptide (pHLIP). Fluorescent flow cytometry, laser confocal scanning microscopy and transmission electron microscopy data proved that pHLIP-conjugated MNPs interacted with 4T1 cells in two-dimensional culture and in spheroids more effectively at pH 6.4 than at pH 7.2, and entered the cell via clathrin-independent endocytosis. The accumulation efficiency of pHLIP-conjugated MNPs in 4T1 tumors after their intravenous injection, monitored in vivo by magnetic resonance imaging, showed variation. Analysis of the tumor pH profiles recorded with implementation of original nanoprobe pH sensor, revealed obvious correlation between pH measured in the tumor with the amount of accumulated MNPs.

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2.
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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3.
Инвентарный номер: нет.
   
   T 80

   
    Toxicity of Triazavirin, a Novel Russian Antiinfluenza chemotherapeutic [Электронный ресурс] / S. A. Loginova, S. V. Borisevich, V. L. Rusinov, E. N. Ulomskii, V. N. Charushin, O. N. Chupakhin // Antibiotiki i Khimioterapiya . - 2012. - Vol.57, №11-12. - 8-10.
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
MICE -- TOXICITY -- TRIAZAVIRIN
Аннотация: The study of the toxicity of triazavirin, a new antiinfluenza agent, showed that the maximum concentration of the drug, inducing no microscopically visible changes in the structure of the monolayer and the cells of the MDCK and SKEV cell cultures, was 128 and 100 mcg/ml respectively. The maximum drug dose for single intraperitoneal administration inducing no signs of acute intoxication in albino mice weighing 10-12 g was 1000 mg/kg. In investigation of the chronic toxicity it was shown that oral administration of the drug (by 0.05 ml) to the albino mice in a dose of 200 mg/kg (maximum possible concentration by the solubility) daily for 10 days was well tolerated by the laboratory animals. The maximum tolerable dose of triazavirin for the albino mice was >200 mg/kg.

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4.
Инвентарный номер: нет.
   
   T 44

    Rusinov, V. L.
    The scintillator tile hadronic calorimeter prototype [Text] / V. L. Rusinov // Nuclear Physics B, Proceedings Supplements. - 2006. - Vol. 150: Innovative Particle and Radiation Detectors. - P253-256
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: A high granularity scintillator hadronic calorimeter prototype is described. The calorimeter is based on a novel photodetector - Silicon Photo-Multiplier (SiPM). The main parameters of SiPM are discussed as well as readout cell construction and optimization. The experience with a small prototype production and testing is described. A new 8 k channel prototype is being manufactured now.

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5.
Инвентарный номер: нет.
   
   T 44

   
    The effect of mustard gas on the biological activity of soil [Text] / N. Medvedeva, Yu. Polyak, I. Kuzikova, O. Orlova, G. Zharikov // Environmental Research. - 2008. - Vol. 106, № 3. - P289-295
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: A special group of substances that are very dangerous for the biosphere includes war gases such as mustard gas (bis(2-chloroethyl)sulphide). The influence of mustard gas hydrolysis products (MGHPs) on soil microbiota has been investigated. These substances bear numerous toxic effects on soil microorganisms. They change significantly the number and the specific composition of soil microbiota and inhibit the enzyme activity of soils. The main "ecological targets" of mustard and its hydrolysis products' toxic action have been determined. MGHPs affect the growth and reproduction of soil micromycetes, as well as their morphological and cultural properties. Increase in number and size of mitochondria in the fungal cells is accompanied by increase in dehydrogenases activity. Cell permeability influenced by MGHPs grows in connection with concentration of toxicants. Increase of permeability corresponds to growth of the amount of unsaturated fatty acids. The changes in the fatty acid composition of lipids in the cells of the soil micromycetes display their adaptation to adverse impact of the substances studied. MGHPs and thiodiglycol enhance synthesis of polysaccharides and pigments.

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6.
Инвентарный номер: нет.
   
   S 98

   
    Synthesis, transformation and biological evaluation of 2,3-secotriterpene acetylhydrazones and their derivatives [Electronic resource] / V. V. Grishko, I. A. Tolmacheva, N. V. Galaiko, A. V. Pereslavceva, L. V. Anikina, L. V. Volkova, B. A. Bachmetyev, P. A. Slepukhin // European Journal of Medicinal Chemisrty. - 2013. - Vol.68. - С. 203-211. - Bibliogr. : p. 211 (34 ref.)
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
ANTIVIRAL ACTIVITY -- ACETYLHYDRAZONE -- BETULONIC ACID
Аннотация: It has been previously shown that semi-synthetic A-secotriterpene acetylhydrazones of 1-cyano-28-methoxy-28-oxo-2,3-seco-2-norlup-20(29)-en-3-al and 1-cyano-2,3-seco-2-nor-19β,28-epoxy-18αH-olean-3-al (1, 2) inhibit the vesicular stomatitis virus (VSV) replication. To improve the antiviral activity against VSV, structural modifications of compounds 1 and 2 were performed, and new A-secoderivatives containing the acetylhydrazone fragment were obtained from betulonic acid and its methyl ester, allobetulone, and 3-oxo-18βH-glycyrrhetinic acid methyl ester. The inhibitory effects of these compounds on VSV replication in porcine embryo kidney (PEK) cells were determined after infection. It was shown that introduction of the 3′-acetyl-5′-methyl-1′,3′,4′-oxadiazoline fragment into lupane triterpene structures lead to an increase in the antiviral activity of A-secotriterpene derivatives. However, the presence of a heterocyclic moiety enhanced toxic activity and reduced the therapeutic indices of these agents. Investigation in the anti-proliferative activity of the heterocyclic derivatives has shown high sensitivity of A-549, MS and RD tumor cell lines to lupane (R)-oxadiazoline 11a. The pro-apoptotic effect of 11a was confirmed by the AnnexinV/PI analysis

\\\\expert2\\NBO\\European Journal of Medicinal Chemistry\\2013, v.68, p.203.pdf
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7.
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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8.
Инвентарный номер: нет.
   
   S 98

   
    Synthesis of Triterpene A-Condensed Azoles [Electronic resource] / N. V. Galaiko, A. V. Nazarov, I. A. Tolmacheva, P. A. Slepukhin, Y. B. Vikharev, O. A. Maiorova, V. V. Grishko // Chemistry of Heterocyclic Compounds. - 2014. - Article in Press
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
ALFA-HYDROXIMINO KETONES -- 1,2,3-TRIAZOLES -- ALLOBETULONE
Аннотация: Lupane and 18αH-oleanane α-hydroximino ketones were used to synthesize derivatives condensed at ring A with a substituted azole fragment, namely, C(2)-C(3)-fused oxazoles and 1,2,3-triazoles. Triterpene isoxazoles fused at the C(1)-C(2) bond are described for the first time. An optimized method was proposed for the synthesis of unsubstituted 1,2,3-triazoles, displaying cytotoxic activity (IC50 8.4-40.7 μM) relative to rhabdomyosarcoma, lung carcinoma, and MS melanoma cell lines.

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9.
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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10.
Инвентарный номер: нет.
   
   S 98

   
    Synthesis and Crystal Structure of (S)-2-((S)-2-(N-Ts-Amino)-3-methylbutanoyl)-3-(1H-indol-3-yl)-6-phenyl-3,4-dihydro-1,2,4-triazin-5(2H)-one [Electronic resource] / I. N. Egorov, V. L. Rusinov, P. A. Slepukhin, O. N. Chupakhin // Journal of Chemical Crystallography . - 2010. - Vol. 40, № 4. - P387-390
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: The diastereoselective synthesis, NMR and X-ray structure of (S)-2-((S)-2-(N-Ts-amino)-3-methylbutanoyl)-3-(1H-indol-3-yl)-6-phenyl-3,4-dihydro-1,2,4-triazin-5(2H)-one—a potential antivirus agent are reported. The compound crystallizes in the triclinic space group P1 with unit cell parameters: a = 5.9259(6) A, b = 9.6370(12) A, c = 12.9541(9) A, = 109.210(9)°, beta = 90.804(7)°, y = 105.074(10)° and Z = 1.

\\\\Expert2\\nbo\\Journal of Chemical Crystallography\\2010.v.40, N 4, p.387.pdf
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