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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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11.
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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12.
Инвентарный номер: нет.
   
   S 98


   
    Synthesis and antiviral activity of fluorinated 3-phenyl-1,2,4-benzotriazines [Electronic resource] / S. K. Kotovskaya, G. A. Zhumabaeva, N. M. Perova, Z. M. Baskakova, V. N. Charushin, O. N. Chupakhin, E. F. Belanov, N. I. Bormotov, S. M. Balakhnin, O. A. Serova // Pharmaceutical Chemistry Journal. - 2007. - Vol. 41, № 2. - P62-68. - Библиогр. : с. 68 (18 назв.)
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
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. ??

\\\\Expert2\\nbo\\Pharmaceutical Chemistry Journal\\2007, 41 (2), 62.pdf
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13.
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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14.
Инвентарный номер: нет.
   
   S 98


   
    Synthesis and antitumor activity of fluorinated derivatives of [i,j]-annelated quinolones [Electronic resource] / G. N. Lipunova, E. V. Nosova, L. P. Sidorova, V. N. Charushin // Pharmaceutical Chemistry Journal. - 2011. - Vol. 45, № 4. - P208-210 : ил. - Bibliogr. : p. 210 (7 ref.)
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: Tri- and pentacyclic fluoroquinolones were synthesized by intramolecular cyclization of the corresponding 3-hydrazinopolyfluorobenzoylacrylates followed by substitution of fluorine atoms by amine residues. The antitumor activity of the resulting compounds was studied at the National Cancer Institute using cultures of 60 cell lines of nine groups, including leukemia, lung tumor, large intestine tumor, CNS tumor, melanoma, ovary tumor, renal tumor, prostate tumor, and breast tumor. Relationships between structure and antitumor activity were analyzed. In vivo experimental data from hollow fiber tests are presented for two derivatives

\\\\Expert2\\nbo\\Pharmaceutical Chemistry Journal\\2011, 45 (4), 208.pdf
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15.
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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16.
Инвентарный номер: нет.
   


   
    Pyrrolylquinoxaline-2-one derivative as a potent therapeutic factor for brain trauma rehabilitation / E. A. Dutysheva, M. A. Mikeladze, N. D. Aksenov [и др.] // Pharmaceutics. - 2020. - Vol. 12, № 5. - С. 414
Кл.слова (ненормированные):
APOPTOSIS -- CEREBROSPINAL FLUID -- HSP70 -- SMALL MOLECULE -- TRAUMATIC BRAIN INJURY
Аннотация: Traumatic brain injury (TBI) often causes massive brain cell death accompanied by the accumulation of toxic factors in interstitial and cerebrospinal fluids. The persistence of the damaged brain area is not transient and may occur within days and weeks. Chaperone Hsp70 is known for its cytoprotective and antiapoptotic activity, and thus, a therapeutic approach based on chemically induced Hsp70 expression may become a promising approach to lower post-traumatic complications. To simulate the processes of secondary damage, we used an animal model of TBI and a cell model based on the cultivation of target cells in the presence of cerebrospinal fluid (CSF) from injured rats. Here we present a novel low molecular weight substance, PQ-29, which induces the synthesis of Hsp70 and empowers the resistance of rat C6 glioma cells to the cytotoxic effect of rat cerebrospinal fluid taken from rats subjected to TBI. In an animal model of TBI, PQ-29 elevated the Hsp70 level in brain cells and significantly slowed the process of the apoptosis in acceptor cells in response to cerebrospinal fluid action. The compound was also shown to rescue the motor function of traumatized rats, thus proving its potential application in rehabilitation therapy after TBI.

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17.
Инвентарный номер: нет.
   
   P 58


   
    Photophysics, photochemistry and bioimaging application of 8-azapurine derivatives / A. K. Eltyshev, I. A. Agafonova, A. S. Minin [et al.] // Organic & biomolecular chemistry. - 2021. - Vol. 19, № 45. - P9880-9896
ББК Г
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: New 2-aryl-1,2,3-triazolopyrimidines were designed, synthesized, and characterized. Their optical properties were thoroughly studied in the solid phase, in solution and in a biological environment. Density Functional Theory (DFT) based calculations were performed, including the molecular geometry optimization for both the ground state and the first singlet excited state, the prediction of the UV-Vis absorption and fluorescence spectra, the determination of the molecular electrostatic properties and the solvent effect on the optical properties. The emission intensity was revealed to increase in time upon irradiation. Mass spectrometric research, quantum mechanical calculations, and analysis of literature data suggested a possible photo-transformation pathway through the homolytic cleavage of one of the C–Cl bonds upon irradiation with UV light. The structure of the active intermediate was identified by the series of mass spectrometry experiments and via synthesis of putative transformation products. The kinetic parameters measured in different solvents allowed estimating the rate of these photo-transformations. Biological experiments demonstrated that 2-aryl-1,2,3-triazolopyrimidines penetrate cells and selectively accumulate in the cell membrane and the Golgi complex and endoplasmic reticulum. Their unique properties pave the way for new possible applications of fluorescent 8-azapurines in biology and medicine.

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18.
Инвентарный номер: нет.
   


   
    Modification of chemically and physically obtained Fe3O4 magnetic nanoparticles with L-Lys for cell labeling / A. M. Demin, O. F. Kandarakov, A. S. Minin [et al.] // Russian chemical bulletin. - 2021. - Vol. 70, № 6. - P1199-1208
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: Peculiar features of the modification of Fe3O4 magnetic nanoparticles (MNPs) obtained by co-precipitation from solutions of FeII and FeIII salts (10-nm MNPs) and by the gas-condensation method (30-nm MNPs) with 3-aminopropylsilane and then with L-lysine were studied. The chemically obtained MNPs possess more pronounced hydrophilic properties and therefore readily form stable aqueous colloidal solutions and can be loaded with a larger amount of L-Lys. However, samples based on the physically obtained MNPs were characterized by more efficient internalization and longer retention times by the NIH 3T3 cells. The results obtained can be used in the design of novel nanomaterials for magnetic cell labeling.

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19.
Инвентарный номер: нет.
   


    Rammohan, A.
    Minireview: Remdesivir, a prominent nucleotide/nucleoside antiviral drug / A. Rammohan, G. V. Zyryanov // Polycyclic aromatic compounds. - 2021. - Vol. 42, № 8. - P5824-5831
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
ANTIVIRAL DRUG -- NUCLEOTIDE ANALOGUE -- REMDESIVIR
Аннотация: Nucleotide analogues are the divergent scaffolds that are reliable potential therapeutic drugs to treat the wide range of diseases including viral infections. For instance, Remdesivir is a biologically important nucleotide analogue prodrug that can act as a key drug target for the diseases Ebola and COVID-19. Remdesivir is a structurally chiral aryloxy-phosphoramidate prodrug as it is metabolized into nucleoside triphosphate (active drug form) inside the cell through sequential reactions by ester mediated-hydrolysis. Thus, the current minireview focuses on the earlier reported synthetic approaches of key fragments of remdesivir and their developments to attain the scale-up yields of the drug for clinical/commercial applies. Further, this review serves as a template for the design and development of other complex organic molecules.

https://doi.org/10.1080/10406638.2021.1947331
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20.
Инвентарный номер: нет.
   
   H 86


    Hristov, P. K.
    Lipid peroxidation induced by ultrasonication in Ehrlich ascitic tumor cells [] / P. K. Hristov, L. A. Petrov, E. M. Russanov // Cancer Letters. - 1997. - Vol.121, N1. - С. 7-10
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: The mechanism of sonodynamic action in tumor cells is poorly investigated. It is known that ultrasound generates free radicals in phosphatidylcholine liposomes used as a membrane model. The participation of lipid peroxidation products in the mechanisms of physiological suppression of cell multiplication has been investigated for some tumor cells

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