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Труды сотрудников ЦНБ УрО РАН
Публикации Черешнева В.А.
Публикации Чарушина В.Н.
Каталог библиотеки ИГД УрО РАН
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Электронная энциклопедия «Дискурсология»
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 Найдено в других БД:Каталог книг и продолжающихся изданий (1)Публикации Черешнева В.А. (2)Публикации Чарушина В.Н. (8)
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 1-10    11-14 
1.

Вид документа : Статья из журнала
Шифр издания : 54/F 70
Автор(ы) : Pokrovskii A. G., Il"ichyova E.A., Kotovskaya S. K., Romanova S. A., Charushin V. N., Chupakhin O. N.
Заглавие : Fluorinated derivatives of benz[4,5]imidazo[2,1-b][1,3]thiazoles are inhibitors of measles viruses
Место публикации : Doklady Akademii Nauk . - 2004. - Vol.398, №3. - С. 412-414
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): antiviral activity--cytotoxicity--fluorinated benzimidazoles
Аннотация: The results of in vitro anti-virus activity investigation for the new benzimidazoles (their synthesis is reported previously) are presented. The activity of the most active compound was studied in dependence of its introduction to the culture (before virus adsorption, simultaneously with virus, directly after virus adsorption, after 6 hours and after 1 day). Preliminary treatment of cells didn't protect them from further infecting; therewith the compound introduction simultaneously with virus or after infection caused no considerable effect on its anti-virus activity. The latter is attributed to blocking of late stages of measles virus reproduction - synthesis or arrangement of virus proteins
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2.

Вид документа : Статья из журнала
Шифр издания : 54/S 98
Автор(ы) : Kotovskaya S. K., Baskakova Z. M., Charushin V. N., Chupakhin O. N., Belanov E. F., Bormotov N. I., Balakhnin S. M., Serova O. A.
Заглавие : Synthesis and antiviral activity of fluorinated pyrido[1,2-a]benzimidazoles [Electronic resource]
Место публикации : Pharmaceutical Chemistry Journal. - 2005. - Vol. 39, № 11. - С. 574-578
Систем. требования: http://www.springerlink.com/content/58722p2385288304/fulltext.pdf
Примечания : Библиогр. : с. 578 (16 назв.). - 1.11.2011 г.
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: Methods for the synthesis of fluorinated pyrido[1,2-a]benzimidazoles have been developed, and a series of such compounds has been obtained and studied for biological activity. In particular, 5,6-difluoro-2-cyanobenzimidazole (II) was synthesized for the first time using the reaction of 1,2-diamino-4,5-difluorobenzole (I) with cyanoacetic ether. Pyrido[1,2-a]benzimidazoles (III, IV) were obtained via condensation of benzimidazole II with diethylethoxymethylene malonate and ethyl acetoacetate. The synthesized pyrido[1,2-a]benzimidazoles (III–XIII) were subjected to screening on a culture of Vero cells for antiviral activity and cytotoxicity with respect to ortho-poxviruses that are pathogenic for humans. ??
\\\\Expert2\\nbo\\Pharmaceutical Chemistry Journal\\2005, 39 (11),574.pdf
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3.

Вид документа : Статья из журнала
Шифр издания : 54/S 98
Автор(ы) : Kotovskaya S. K., Zhumabaeva G. A., Perova N. M., Baskakova Z. M., Charushin V. N., Chupakhin O. N., Belanov E. F., Serova O. A.
Заглавие : Synthesis and antiviral activity of fluorinated 3-phenyl-1,2,4- benzotriazines
Место публикации : Pharmaceutical Chemistry Journal. - 2007. - Vol.41, №2. - С. 62-68
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): cyclization--cytotoxicity--fluorination
Аннотация: New synthetic approaches to fluorinated 3-phenyl-1,2,4-benzotriazines for biological testing have been elaborated. 1-(3,4-Difluorophenyl)-3,5- diphenylformazan (IVa) was synthesized via dinitriding of 3,4-difluoroaniline, followed by azo-addition of the resulting azobenzenediazonium chloride with acetaldehyde phenylhydrazone. 6,7-Difluoro-3-phenyl-1,2,4-benzotriazine (Va) was obtained via intramolecular cyclization of formazan IVa in the presence of BF3/AcOH complex. Monofluoro-substituted 6-R-7-fluoro-3-phenyl-1,2,4- benzotriazine derivatives (Vb-Vq) were prepared by substituting fluorine atom with alkoxides in 3,4-difluoronitrobenzene. Conditions for nucleophilic substitution of the second fluorine atom in benzotriazines V have been established. Fluorinated 3-phenyl-1,2,4-benzotriazines have been tested for antiviral and cytotoxic activity on Vero cell cultures and proved to be active against severe diseases caused by smallpox and some other pathogenic viruses
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4.

Вид документа : Статья из журнала
Шифр издания : 54
Автор(ы) : Deev S. L., Yasko M. V., Karpenko I. L., Ulomskii E. N., Chupakhin O. N.
Заглавие : 1,2,4-Triazoloazine derivatives as a new type of herpes simplex virus inhibitors
Место публикации : Bioorganic Chemistry . - 2010. - Vol. 38, № 6. - С. 265-270
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: A new class of inhibitors of herpes simplex virus replication was found. The compounds under study are derived from condensed 1,2,4-triazolo[5,1-c][1,2,4]triazines and 1,2,4-triazolo[1,5-a]pyrimidines, structural analogues of natural nucleic bases. Antiherpetic activity and cytotoxicity of the compounds were studied. The corresponding triphosphates of several active compounds were prepared and tested as inhibitors of DNA synthesis catalyzed by herpes simplex virus polymerase. The potential mechanism of their action is blocking of DNA dependent DNA polymerase, a key enzyme of viral replication
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5.

Вид документа : Статья из журнала
Шифр издания : 54/C 51
Автор(ы) : Konstantinova I. D., Selezneva O. M., Fateev I. V., Balashova T. A., Kotovskaya S. K., Baskakova Z. M., Charushin V. N., Mikhailopulo I. A.
Заглавие : Chemo-enzymatic synthesis and biological evaluation of 5,6-disubstituted benzimidazole ribo- and 2′-deoxyribonucleosides
Место публикации : Synthesis (Germany). - 2013. - Vol.45, №2, art. N SS-2012-T0784-OP. - С. 272-280
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): 5,6-disubstituted benzimidazoles--nucleosides--substrate properties
Аннотация: A number of new 5,6-disubstituted benzimidazoles have been prepared and their substrate properties for recombinant E. coli purine nucleoside phosphorylase (PNP; the product of the deoD gene) in the transglycosylation reaction were investigated. The heterocyclic bases showed good substrate activity for PNP and the ribo- and 2-deoxyribonucleosides were synthesized. The predominant (OMe and OEt) or exclusive (Oi-Pr, morpholino, and N-methylpiperazino) formation of the 5-substituted 6-fluoro-1-(β-d- ribofuranosyl)benzimidazoles was observed. The formation of the regioisomeric 6- methoxy-, 6-ethoxy-, or 6-isopropoxy-substituted 1-(2-deoxy-β-d- ribofuranosyl)-5-fluorobenzimidazoles was observed in the trans-2- deoxyribosylation reaction of the corresponding bases. The predominant or exclusive formation of the regioisomeric N1-nucleosides with bulky 5-substituents of 6-fluorobenzimidazole points to a large hydrophobic pocket in the E. coli PNP active site that can accommodate these groups. The biological activity of the synthesized nucleosides was studied and revealed no inhibitory activity against a broad variety of DNA and RNA viruses. The compounds also lacked significant cytotoxicity
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6.

Вид документа : Статья из журнала
Шифр издания : 54/C 51
Автор(ы) : Kharitonova M. I., Fateev I. V., Kayushin A. L., Konstantinova I. D., Kotovskaya S. K., Andropova V. L., Galegov G. A., Charushin V. N., Miroshnikov A. I.
Заглавие : Chemoenzymatic Synthesis and Antiherpes Activity of 5-Substituted 4,6-Difluorobenzimidazoles Ribo- and 2′-Deoxyribonucleosides [Электронный ресурс]
Место публикации : Synthesis (Germany). - 2016. - Vol. 48, № 3. - С. 394-406
Систем. требования: https://www.thieme-connect.com/products/ejournals/html/10.1055/s-0035-1560911
Примечания : Bibliogr. : p. 405-406 (37 ref.). - 29.03.16
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): 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.

Вид документа :
Шифр издания : Г/U 61
Автор(ы) : Khamidullina L. A., Puzyrev I. S., Slepukhin P. A., Pestov A. V., Tobysheva P. D., Burygin G. L., Dorovatovskii P. V., Zubavichus Y. V., Mitrofanova A. V., Khrustalev V. N., Tskhovrebov A. G., Timofeeva T. V., Solari E., Nenajdenko V. G.
Заглавие : Unsymmetrical trifluoromethyl methoxyphenyl β-diketones: effect of the position of methoxy group and coordination at Cu(II) on biological activity
Место публикации : Molecules. - 2021. - Vol. 26, № 21. - Ст.6466
ББК : Г
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): 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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8.

Вид документа : Статья из журнала
Шифр издания :
Автор(ы) : Dutysheva E. A., Utepova I. A., Trestsova M. A., Anisimov A. S., Charushin V. N., Chupakhin O. N., Margulis B. A., Guzhova I. V., Lazarev V. F.
Заглавие : Synthesis and approbation of new neuroprotective chemicals of pyrrolyl- and indolylazine classes in a cell model of Alzheimer's disease
Место публикации : European journal of medicinal chemistry. - 2021. - Vol. 222. - С. 113577
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): pyrrolylazines--neuroprotectors--chaperones--amyloid-beta--alzheimer's disease
Аннотация: One of the major causes of neurodegeneration in the pathogenesis of Alzheimer's disease is the accumulation of cytotoxic amyloid species within the intercellular compartments of the brain. The efficacy of the anti-proteotoxic mechanism based on the molecular chaperones Hsp70 and Hsp90 in numerous types of neurons is often low, while its pharmacological enhancement has been shown to ameliorate the physiological and cognitive functions of the brain. Suggesting that the chemicals able to induce heat shock protein synthesis and therefore rescue neural cells from cytotoxicity associated with amyloid, we have synthesized a group of pyrrolyl- and indolylazines that cause the accumulation of heat shock proteins, using a novel method of photocatalysis that is employed in green chemistry. The selected compounds were tested in a cell model of Alzheimer's disease and demonstrated a pronounced neuroprotective effect. These substances increased the survival of neurons, blocked the activation of β-galactosidase, and prevented apoptosis in neurons cultured in the presence of β-amyloid.
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9.

Вид документа : Статья из журнала
Шифр издания :
Автор(ы) : Bratskaya S., Skatova A., Privar Y., Boroda A., Kantemirova E., Maiorova M., Pestov A.
Заглавие : Stimuli-responsive dual cross-linked N-carboxyethylchitosan hydrogels with tunable dissolution rate
Место публикации : Gels. - 2021. - Vol. 7, № 4. - Ст.188
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): 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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10.

Вид документа : Статья из журнала
Шифр издания :
Автор(ы) : Varaksin M. V., Smyshliaeva L. A., Rusinov V. L., Melekhin V. V., Charushin V. N., Chupakhin O. N., Makeev O. G., Baldanshirieva A. D., Gubina O. G.
Заглавие : Synthesis, characterization, and in vitro assessment of cytotoxicity for novel azaheterocyclic nido-carboranes – Candidates in agents for boron neutron capture therapy (BNCT) of cancer
Место публикации : Tetrahedron. - 2021. - Vol. 102. - С. 132525
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): 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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