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1.

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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2.

Вид документа : Статья из журнала
Шифр издания :
Автор(ы) : Shabunina O. V., Starnovskaya E. S., Shaitz Y. K., Kopchuk D. S., Sadieva L. K., Taniya O. S., Nikonov I. L., Santra S., Zyryanov G. V., Charushin V. N., Kim G. A.
Заглавие : Asymmetrically substituted 5,5′′-diaryl-2,2′:6′,2′′-terpyridines as efficient fluorescence “turn-on” probes for Zn2+ in food/cosmetic samples and human urine
Место публикации : Journal of photochemistry and photobiology A: Chemistry. - 2021. - Vol. 408. - С. 113101
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
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3.

Вид документа : Статья из журнала
Шифр издания : 54/A 10
Автор(ы) : Sarkar A., Santra S., Kundu S. K. , Zyryanov G. V., Chupakhin O. N., Charushin V. N., Majee A.
Заглавие : A decade update on solvent and catalyst-free neat organic reactions: a step forward towards sustainability [Электронный ресурс]
Место публикации : Green Chemistry. - 2016. - Vol. 18, № 16. - С. 4475-4525
Систем. требования: http://apps.webofknowledge.com/full
Примечания : 26.10.16
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): one-pot synthesis --diels-alder reactions--electron-deficient olefins
Аннотация: Particular success has been achieved in the synthesis of new products and in processes since the twelve principles of "green chemistry" were formulated in the 1990s. These products and processes are more compatible with human health, society, and the environment. In this review, a collection of research reports have been documented from the viewpoint of green chemistry. The main theme of this review is neat reactions, which are solvent and catalyst-free reactions. Neat reactions in the absence of any solvent or catalyst with concise summaries of microwave, ball milling, and neat reactions have been described.
\\\\expert2\\NBO\\Green Chemistry\\2016, v.18, N 16, p.4475.pdf
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4.

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 : Dataset of NMR-spectra pyrrolyl- and indolylazines and evidence of their ability to induce heat shock genes expression in human neurons
Место публикации : Data in Brief. - 2021. - № 39. - С. 107562
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): pyrrolylazines--indolylazines--photocatalysis--nuclear magnetic resonance--green chemistry
Аннотация: These data are related to our previous paper “Synthesis and approbation of new neuroprotective chemicals of pyrrolyl-and indolylazine classes in a cell model of Alzheimer’s disease” (Dutysheva et al., 2021), in which we demonstrate neu-roprotective abilities of pyrrolyl- and indolylazines in a cell model of Alzheimer’s disease. Using a novel procedure of photocatalysis we have synthesized a group of new compounds. The current article presents nuclear magnetic resonance spectra including heteronuclear single quantum coherence spectra of chemicals synthesized by us. The effect of new compounds have on heat shock proteins genes expression in reprogrammed human neurons are presented. We also presented data that verify neuronal phenotype of reprogrammed cells.
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5.

Вид документа : Статья из журнала
Шифр издания :
Автор(ы) : Pershina A. G., Demin A. M., Perekucha N. A., Brikunova O. Y., Efimova L. V., Nevskaya K. V., Vakhrushev A. V., Zgoda V. G., Uimin M. A., Minin A. S., Malkeyeva D., Kiseleva E., Zima A. P., Krasnov V. P., Ogorodova L. M.
Заглавие : Peptide ligands on the PEGylated nanoparticle surface and human serum composition are key factors for the interaction between immune cells and nanoparticles
Место публикации : Colloids and Surfaces B: Biointerfaces. - 2023. - Vol. 221. - С. 112981
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: The architecture of a nanoparticles' surface formed due to a modification with a ligand and protein corona formation in biofluids is critical for interactions with cells in vivo. Here we studied interactions of immune cells with magnetic nanoparticles (MNPs) covalently modified with polyethylene glycol (PEG) and their counterparts conjugated with peptides: a pH (low) insertion peptide (pHLIP) and cycloRGD as a targeting ligand in human serum. The conjugation of MNPs-PEG with pHLIP, but not with cycloRGD, enhanced the association of these particles with mononuclear phagocytic cells in vitro and in vivo. We did not find a clear difference in protein corona composition between the pHLIP-modified and parental PEGylated nanoparticles. Analysis of the effect of autologous human serum on MNP uptake by monocytes showed that the efficiency of endocytosis varies among healthy donors and depends on intrinsic properties of serum. Nevertheless, using classic blood, coagulation, biochemical tests, and anti-PEG IgG serum level, we failed to identify the cause of the observed interdonor variation. These individual differences should be taken into consideration during testing of nanotherapeutics.
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6.

Вид документа : Статья из журнала
Шифр издания :
Автор(ы) : Volobueva A. S., Zarubaev V. V., Fedorchenko T. G., Lipunova G. N., Tungusov V. N., Chupakhin O. N.
Заглавие : Antiviral properties of verdazyls and leucoverdazyls and their activity against group b enteroviruses
Место публикации : Russian journal of infection and immunity. - 2023. - Vol. 13, № 1. - С. 107-118
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
ЗДРАВООХРАНЕНИЕ. МЕДИЦИНСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): enteroviruses--enteroviral infection--coxsackievirus
Аннотация: Enteroviruses are non-enveloped viruses of Enterovirus genus, Picornaviridae family, causing a variety of human diseases: from acute respiratory and intestinal infections to more severe pathologies including poliomyelitis, encephalitis, myocarditis, pancreatitis. Currently, no approved direct-acting antiviral drugs for treatment of enterovirus infections exists, whereas vaccination is available only for prevention of poliomyelitis and enterovirus 71 infection. Therefore, it is promising to conduct a search for inhibitors of enteroviruses life cycle in drug development to treat enterovirus infections. Here, antiviral properties of stable free radicals, verdazyls, and their precursors, leucoverdazyls, were investigated. It has been shown that leucoverdazyls vs verdazyls increased the survival of permissive cell culture infected with coxsackievirus. The activity range of the lead leucoverdazyl against RNA-containing and DNA-containing human viruses (in the viral yield reduction assay) and its proposed mechanism of action (time of addition assay) was studied. The lead compound suppressed reproduction of group B enteroviruses in vitro, with modest activity against influenza A virus and no activity against herpes virus type 1 and adenovirus type 5. The maximum decrease in viral titers was observed upon its addition to infected cells during early and middle stages of the virus life cycle. Thus, we concluded that the studied compound has a pronounced inhibitory activity against group B enteroviruses not belonging to the class of capsid binder inhibitors, without virucidal properties. Previously, we described antioxidant properties of leucoverdazyls. It is known that many viral infections are accompanied by production of reactive oxygen species and oxidative stress, and some compounds with antioxidant properties exhibit antiviral potential. Targeted chemical modifications of leucoverdazyls and further studies of leucoverdazyl mechanism of action as well as in vivo animal studies are needed. However, the results obtained may be useful for future development of new antiviral drugs to treat enteroviral infections.
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7.

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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8.

Вид документа : Статья из журнала
Шифр издания : 54/A 62
Автор(ы) : Karpenko I. L., Deev S. L., Kiselev O. I., Charushin V. N., Rusinov V. L., Ulomskii E. N., Deeva E.G., Kukhanova M. K.
Заглавие : Antiviral properties, metabolism, and pharmacokinetics of a novel azolo-1,2,4-triazine-derived inhibitor of influenza A and B virus replication
Место публикации : Antimicrobial Agents and Chemotherapy . - 2010. - Vol.54, №5. - С. 2017-2022
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): animal cell--animal experiment--antiviral activity
Аннотация: Influenza viruses of types A and B cause periodic pandemics in the human population. The antiviral drugs approved to combat influenza virus infections are currently limited. We have investigated an effective novel inhibitor of human influenza A and B viruses, triazavirine {2-methylthio-6-nitro-1,2,4- triazolo[5,1-c]-1,2,4-triazine-7(4Í)-one} (TZV). TZV suppressed the replication of influenza virus in cell culture and in chicken chorioallantoic membranes, and it protected mice from death caused by type A and B influenza viruses. TZV was also effective against a rimantadine-resistant influenza virus strain and against avian influenza A virus H5N1 strains. The pharmacokinetic parameters and bioavailability of TZV were calculated after the administration of TZV to rabbits. The TZV metabolite AMTZV {2-methylthio-6-amino-1,2,4- triazolo[5,1-s]-1,2,4-triazin(e)-7(4Í)-one} was discovered inÍÅK 293T and Huh7 cell cultures, a liver homogenate, and rabbit blood after intragastric administration of TZV. AMTZV was nontoxic and inactive as an inhibitor of influenza virus in cell culture. Most likely, this metabolite is a product of TZV elimination
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9.

Вид документа : Статья из журнала
Шифр издания : 54/A 62
Автор(ы) : Karpenko I. L., Deev S. L., Kiselev O. I., Charushin V. N., Rusinov V. L., Ulomskii E. N., Deeva E.G., Chupakhin O. N.
Заглавие : Antiviral Properties, Metabolism, and Pharmacokinetics of a Novel Azolo-1,2,4-Triazine-Derived Inhibitor of Influenza A and B Virus Replication
Место публикации : Antimicrobial Agents and Chemotherapy. - 2010. - Vol. 54, № 5. - С. 2017-2022
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: Influenza viruses of types A and B cause periodic pandemics in the human population. The antiviral drugs approved to combat influenza virus infections are currently limited. We have investigated an effective novel inhibitor of human influenza A and B viruses, triazavirine {2-methylthio-6-nitro-1,2,4-triazolo[5,1-c]-1,2,4-triazine-7(4I)-one} (TZV). TZV suppressed the replication of influenza virus in cell culture and in chicken chorioallantoic membranes, and it protected mice from death caused by type A and B influenza viruses. TZV was also effective against a rimantadine-resistant influenza virus strain and against avian influenza A virus H5N1 strains. The pharmacokinetic parameters and bioavailability of TZV were calculated after the administration of TZV to rabbits. The TZV metabolite AMTZV {2-methylthio-6-amino-1,2,4-triazolo[5,1-s]-1,2,4-triazin(e)-7(4I)-one} was discovered in IAK 293T and Huh7 cell cultures, a liver homogenate, and rabbit blood after intragastric administration of TZV. AMTZV was nontoxic and inactive as an inhibitor of influenza virus in cell culture. Most likely, this metabolite is a product of TZV elimination
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10.

Вид документа : Статья из журнала
Шифр издания : 54/P 72
Автор(ы) : Vasilyeva T.M., Makarov V. A., Chupakhin O. N., Sidorova L. P., Perova N. M., Rusinov V. L.
Заглавие : Platelet aggregation inhibitor properties of 1,3,4-thiadiazine thiadiazines
Место публикации : Gematologiya i Transfusiologiya . - 2008. - Vol. 53, № 4. - С. 12-15
Примечания : Bibliogr. : p. 15 (14 ref.)
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: Effects of new 1,3,4-thiadiazines on human platelet aggregation were studied in vitro. All 1,3,4-thiadiazines inhibited aggregation induced by ADP and arachidonic acid in a wide range of concentrations. The most active of the studied 1,3,4-thiadiazines were L-19, L-20, L-25, L-28, and L-31 in concentrations of 0.01-1 mM, effectively reducing platelet aggregation induced by arachidonic acid and ADP.
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