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Каталог книг и продолжающихся изданий
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Труды сотрудников ЦНБ УрО РАН
Публикации Черешнева В.А.
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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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Общее количество найденных документов : 14
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1.
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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2.
Инвентарный номер: нет.
   
   S 98

   
    Synthesis and antiviral activity of nonannulated tetrazolylpyrimidines / V. A. Ostrovskii, G. G. Danagulyan, O. M. Nesterova [et al.] // Chemistry of Heterocyclic Compounds. - 2021. - Vol. 57, № 4. - P448–454
УДК
Г
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
PYRIMIDINES -- TETRAZOLES -- BIOLOGICAL ACTIVITY -- LINKERS
Аннотация: Nonannulated tetrazolylpyrimidines in the structure of which the heterocyclic fragments are separated by hydrazinocarbonylmethyl, methylpyrazolyl groups or a sulfur atom were synthesized. Some of these compounds showed moderate in vitro activity against H1N1 subtype of influenza A virus. The selectivity index of the anti-influenza action of {5-[(4,6-dimethylpyrimidin-2-yl)sulfanyl]-1H-tetrazol1-yl}acetic acid, which has very low cytotoxicity, was twice as high as the selectivity index of the reference drug rimantadine.

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3.
Инвентарный номер: нет.
   
   N 89

   
    Novel purine conjugates with N-heterocycles: synthesis and anti-influenza activity / V. P. Krasnov, V. V. Zarubaev, D. V. Gruzdev [et al.] // Chemistry of Heterocyclic Compounds. - 2021. - Vol. 57, № 4. - P498-504
УДК
Г
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
6-CHLOROPURINE -- HETEROCYCLIC AMINES -- ANTIVIRAL ACTIVITY -- INFLUENZA A AND B VIRUSES
Аннотация: A number of novel amides were synthesized by coupling of 6-[(9H-purin-6-yl)amino]hexanoic acid to heterocyclic amines. The antiviral activity of the obtained compounds, as well as of purine conjugates in which 7,8-difluoro-3-methyl-3,4-dihydro-2H-1,4-benzoxazine is linked to position 6 of purine through a fragment of ɷ-amino acids with varying lengths of polymethylene chains against influenza A and B viruses was studied in vitro. Purine derivatives have been shown to have moderate activity against influenza A (H1N1) virus. The antiinfluenza activity and cytotoxicity of conjugates with 7,8-difluoro-3-methyl-3,4-dihydro-2H-1,4-benzoxazine depend on the length of the linker fragment.

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4.
Инвентарный номер: нет.
   

   
    Synthesis and approbation of new neuroprotective chemicals of pyrrolyl- and indolylazine classes in a cell model of Alzheimer's disease / E. A. Dutysheva, I. A. Utepova, M. A. Trestsova [et al.] // European journal of medicinal chemistry. - 2021. - Vol. 222. - P113577
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
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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5.
Инвентарный номер: нет.
   

   
    Chitosan cross-linking with acetaldehyde acetals / A. Pestov, Y. Privar, A. Slobodyuk [et al.] // Biomimetics. - 2022. - Vol. 7, № 1. - Ст. 10
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
CHITOSAN -- ACETALDEHYDE ACETALS -- HYDROGEL
Аннотация: Here we demonstrate the possibility of using acyclic diethylacetal of acetaldehyde (ADA) with low cytotoxicity for the fabrication of hydrogels via Schiff bases formation between chitosan and acetaldehyde generated in situ from acetals in chitosan acetate solution. This approach is more convenient than a direct reaction between chitosan and acetaldehyde due to the better commercial availability and higher boiling point of the acetals. Rheological data confirmed the formation of intermolecular bonds in chitosan solution after the addition of acetaldehyde diethyl acetal at an equimolar NH2: acetal ratio. The chemical structure of the reaction products was determined using elemental analysis and 13C NMR and FT-IR spectroscopy. The formed chitosan-acetylimine underwent further irreversible redox transformations yielding a mechanically stable hydrogel insoluble in a broad pH range. The reported reaction is an example of when an inappropriate selection of acid type for chitosan dissolution prevents hydrogel formation.

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6.
Инвентарный номер: нет.
   

   
    1H-pyrazole-appended pyridines and their 1,2,4-triazine precursors: a rational synthesis and in silico and in vitro evaluation of anti-cancer activity / A. P. Krinochkin, Y. K. Shtaitz, A. K. Rammohan [et al.] // European Journal of Organic Chemistry. - 2022. - Vol. 2022, № 22. - Pe202200227
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: An operationally facile and high yielding one-pot protocol has been developed for the preparation of pyridines appended with pyrazole via NH linker. This protocol includes SNipso/aza-Diels-Alder reactions in up to 54 % yields starting from 1,2,4-triazine precursors. All the synthesized compounds have been evaluated for their in silico activity against JAK1, SYK, and FAK1 kinases. The most promising compound was tested in vitro using A-172, Hs578T, and HepG2 cancer cell lines and exhibited considerable cytotoxicity with IC50 values 50 μM in A-172 and HepG2 cell lines. Anticancer in vitro activity correlates well with the predicted in silico data.

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7.
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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8.
Инвентарный номер: нет.
   
   S 98

   
    Synthesis and antiviral activity of fluorinated 3-phenyl-1,2,4- benzotriazines [Электронный ресурс] / S. K. Kotovskaya, G. A. Zhumabaeva, N. M. Perova, Z. M. Baskakova, V. N. Charushin, O. N. Chupakhin, E. F. Belanov, O. A. Serova // Pharmaceutical Chemistry Journal. - 2007. - Vol.41, №2. - P62-68
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
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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9.
Инвентарный номер: нет.
   

   
    1,2,4-Triazoloazine derivatives as a new type of herpes simplex virus inhibitors [Text] / S. L. Deev, M. V. Yasko, I. L. Karpenko, E. N. Ulomskii, O. N. Chupakhin // Bioorganic Chemistry . - 2010. - Vol. 38, № 6. - P265-270
ББК 54
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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10.
Инвентарный номер: нет.
   
   S 98

   
    Synthesis and antiviral activity of fluorinated pyrido[1,2-a]benzimidazoles [Electronic resource] / S. K. Kotovskaya, Z. M. Baskakova, V. N. Charushin, O. N. Chupakhin, E. F. Belanov, N. I. Bormotov, S. M. Balakhnin, O. A. Serova // Pharmaceutical Chemistry Journal. - 2005. - Vol. 39, № 11. - P574-578. - Библиогр. : с. 578 (16 назв.)
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
SYNTHESIS -- ANTIVIRAL ACTIVITY
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. ??

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