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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 : 54/S 98
Автор(ы) : Pereslavceva A. V., Tolmacheva I. A., Slepukhin P. A., Eltsov O. S., Kucherov I. I. , Eremin V. F., Grishko V. V.
Заглавие : Synthesis of A-Pentacyclic Triterpene α,β-Alkenenitriles [Электронный ресурс]
Место публикации : Chemistry of Natural Compounds. - 2014. - Vol.49, №6. - С. 1059-1066
Систем. требования: http://download.springer.com/static/pdf/917/art%253A10.1007%252Fs10600-014-0822-2.pdf?auth66=1397205289_e2291bf44b21c8d7aca0a675ff76a144&ext=.pdf
Примечания : Bibliogr. : p. 1066 (24 ref.). - 09.04.2014
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): alfa,beta- alkenenitriles--a-seco-triterpenoids--allobetulone
Аннотация: A-seco-triterpenoids with a methylketone group were synthesized from epimeric 3-hydroxy-3-methyl-1-cyano-2,3-seco-triterpenoids of the lupane and 19β,28-epoxy-18αH-oleanane types, which were formed by a Grignard reaction. The resulting methylketones underwent under base-catalysis conditions an intramolecular cyclization to form A-pentacyclic β-substituted alkenenitriles. The synthesized compounds included 3-methyl-1-cyano-19β,28- epoxy-2,3-seco-2-nor-18αH-olean-3-one and methyl 3-methyl-1-cyano-2- norlup-1(3),20(29)-dien-28-oate, which inhibited in vitro reproduction of human immunodeficiency virus type 1.
\\\\expert2\\nbo\\Chemistry of Natural Compounds\\2014, V.49, N6, p.1059.pdf
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3.

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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4.

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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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 : 54/F 97
Автор(ы) : Grishko V. V., Galaiko N. V., Tolmacheva I. A., Kucherov I. I. , Eremin V. F., Boreco E. I., Savinova O. V., Slepukhin P. A.
Заглавие : Functionalization, cyclization and antiviral activity of A-secotriterpenoids [Электронный ресурс]
Место публикации : European Journal of Medicinal Chemisrty. - 2014. - Vol. 83. - С. 601-608
Систем. требования: http://www.sciencedirect.com/science/article/pii/S0223523414000300
Примечания : 14.08.15
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): a-secotriterpenoids --betulin--18βh-glycyrrhetinic acid
Аннотация: Triterpene derivatives with an α,β-alkenenitrile moiety in the five-membered ring A have been synthesized by nitrile anion cyclizations of 1-cyano-2,3-secotriterpenoids. Oxime-containing precursors, 2,3-secointermediates and five-membered ring A products of cyclizations were screened for in vitro antiviral activity against enveloped viruses – influenza A virus and human immunodeficiency virus type I (HIV-1). Lupane ketoxime and the 2,3-secolupane C-3 aldoxime which possess antiviral activities against both influenza A virus (EC50 12.9–18.2 μM) and HIV-1 (EC50 0.06 μM) were the most promising compounds.
\\\\expert2\\nbo\\European Journal of Medicinal Chemistry\\2014, v.83, p.601-608.pdf
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7.

Вид документа : Статья из журнала
Шифр издания : 54/F 97
Автор(ы) : Grishko V. V., Galaiko N. V., Tolmacheva I. A., Savinova O. V., Slepukhin P. A.
Заглавие : Functionalization, cyclization and antiviral activity of A-secotriterpenoids [Электронный ресурс]
Место публикации : European Journal of Medicinal Chemisrty. - 2014. - Vol.83. - С. 601-608
Систем. требования: http://libgen.org/scimag/get.php?doi=10.1016%2Fj.ejmech.2013.12.058
Примечания : Bibliogr. : p. 608 (37 ref.). - 13.08.2014
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): 18βh-glycyrrhetinic acid--a-secotriterpenoids--antiviral activity
Аннотация: Triterpene derivatives with an α,β-alkenenitrile moiety in the five-membered ring A have been synthesized by nitrile anion cyclizations of 1-cyano-2,3-secotriterpenoids. Oxime-containing precursors, 2,3- secointermediates and five-membered ring A products of cyclizations were screened for in vitro antiviral activity against enveloped viruses - influenza A virus and human immunodeficiency virus type I (HIV-1). Lupane ketoxime and the 2,3-secolupane C-3 aldoxime which possess antiviral activities against both influenza A virus (EC50 12.9-18.2 μM) and HIV-1 (EC50 0.06 μM) were the most promising compounds.
\\\\expert2\\nbo\\European Journal of Medicinal Chemistry\\2014, v.83, p.601-608.pdf
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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 : 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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9.

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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10.

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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