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3′-O-Substituted 5-(perylen-3-ylethynyl)-2′-deoxyuridines as tick-borne encephalitis virus reproduction inhibitors
European Journal of Medicinal Chemistry. 2018. Vol. 155. P. 77–83.
Vladimir A. Korshun
series of analogues of potent antiviral perylene nucleoside dUY11 with methylthiomethyl (MTM), azidomethyl (AZM) and HO-C1e4-alkyl-1,2,3-triazol-1,4-diyl groups at 30-O-position as well as the two products of copper-free alkyne-azide cycloaddition of the AZM derivative were prepared and evaluated against tick-borne encephalitis virus (TBEV). Four compounds (4, 6, 8a, 8b) showed EC50 10 nM, thus appearing the most potent TBEV inhibitors to date. Moreover, these nucleosides have higher lipophilicity (clogP) and increased solubility in aq. DMSO vs. parent compound dUY11.
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Belousov Y., Кискин М. А., Sidoruk A. et al., Australian Journal of Chemistry 2022 Vol. 75 No. 9 P. 572–580
Four new complexes [Ln(pfaa)3(H2O)2]n (Ln = Eu (1), Tb (2)) and [Ln2Cd2(pfaa)10 (phen)2(EtOH)2]·2MeCN (Ln = Eu (3), Tb (4), phen = 1,10-phenanthroline) based on pentaphorphenylacetic acid (Hpfaa) have been prepared and completely investigated. The structures of compounds 1 and 3 were studied by single crystal X-ray diffraction analysis: the isostructural complexes 1 and 2 represent ...
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Кубкин Я. В., Российский кардиологический журнал 2026 Т. 31 № 8S
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The electric double layer (EDL) at a single-crystal metal surface is controlled not only by the electrolyte composition and the electrode potential, but also by the atomic structure of the surface itself. This makes the Ag(hkl)/NaF interface a stringent test for continuum theories of the EDL. In the third part of our series, we examine ...
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EEG recordings are often affected by the loss or corruption of individual channels due to electrode detachment, poor scalp contact, or external interference. Such channels must be accurately reconstructed before further analysis. In this study, we investigate Next-Generation Reservoir Computing (NG-RC) as a data-driven approach for reconstructing corrupted EEG channels and compare its performance with ...
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A self-consistent statistical-mechanical theory of the Hall effect in electrolyte solutions is developed by extending the self-consistent Debye–Hückel–Onsager (SCDHO) framework to crossed electric and magnetic fields. The theory incorporates non-local ionic charge distributions via Slater-type form factors, regularizing the Coulomb interaction at short range, and accounts for dielectric friction through ion-specific coefficients, employing experimental values ...
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Novikov A., New Journal of Chemistry 2026 Vol. 50 P. 13931–13957
The rational design of coinage metal nanocarriers requires a mechanistic understanding of metal-drug binding and predictive descriptors that translate molecular interactions into design rules. Using DFT (B3LYP-D3BJ/def2-TZVP, SMD water), we systematically investigated the binding of 5-fluorouracil (5-FU) and levodopa (l-DOPA) to neutral and cationic homo- and heteronuclear dimers of Au, Ag, and Cu (Au2, Ag2, ...
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Lucas J., Hebbar P., Ryabov F. et al., / Series 10.64898/2026.07.21.739710 "10.64898/2026.07.21.739710". 2026.
A pangenome reference overcomes the inherent limitation of any individual reference genome by integrating the variation present in a population. We present the Human Pangenome Reference Consortium’s (HPRC) Release 2 (HPRC2), an openly available, second phase pangenome that is an approximately fivefold expansion in genome number over HPRC Release 1 (HPRC1) and measurable improvement in ...
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Encyclopedia of Ecology, Third Edition, Four Volume Set - with over 300 chapters - once again provides a comprehensive reference work covering the current ideas and practices in ecology.
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Bacterial chromosomes are tightly packed in the cells due to interactions with specific nucleoid-associated proteins. Among them, the IHF protein draws attention due to its presumed influence on intracellular crystallization processes, leading to bacterial resistance to drugs. The crystal structure of the IHF heterodimer is known only in complex with a short DNA fragment, whereas ...
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Musical training has a significant impact on brain organization, leading to functional and structural
adaptations that enhance auditory, visual, motor, and cognitive processes. This study investigates how
extensive musical training shapes functional brain connectivity by comparing professional musicians and
non-musicians. Using EEG phase-locking value (PLV) analysis, we examined neural synchronization across
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Inhibition of the PD-1/PD-L1 axis has become a clinical standard across multiple malignancies, yet durable benefit remains restricted to selected settings, and many biologically rational combinations fail to maintain clinical benefit in late-phase evaluation. This structured, registry-derived narrative review, supported by expert-guided interpretation, was designed to identify the most clinically meaningful development directions among strategies ...
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Composite gel polymer electrolytes based on a perfluorinated sulfonic acid cation-exchange MF-4SC membrane
containing surface-sulfonated nanoparticles of aluminum oxide, cerium (IV) oxide, and titanium oxide (sAl2O3,
sCeO2, and sTiO2, respectively) were prepared by casting from a dispersion in N,N-dimethylformamide and
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solvent uptake, activation energy, lithium ...
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Mikhaylets E. V., Razorenova A. М., Chernyshev V. L. et al., Scientific Reports 2026 Vol. 16 Article 23560
Meditation offers a naturalistic paradigm for studying introspection, yet the neural dynamics of advanced tantric practices remain largely unexplored. Buddhist Highest Yoga Tantra (BHYT) comprises a sequence of eight dissolution stages culminating in the “clear light” state. We recorded EEG during eyes-closed BHYT meditation performed in monasteries and hermitages (51 sessions from 36 male practitioners; ...
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We present two models with explicit long-range electrostatics in the form of Coulomb interactions. Both models include point charges depending on their local atomic environments, and the second model also conserves a total charge of an atomic system. We combine the proposed long-range models with the local moment tensor potential (MTP) and demonstrate that they ...
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Sun Z., Khvostikov A., Krylov A. et al., Machine Learning and Knowledge Extraction 2026 Vol. 8 No. 1 Article 8
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Turkina A., Vinogradova O., Lomaia E. et al., Annals of Hematology 2025 Vol. 104 P. 2707–2715
Vamotinib (PF-114) is a 3rd -generation, ATP-competitive oral tyrosine kinase inhibitor (TKI) active against wild-type and mutated BCR::ABL1 isoforms including BCR::ABL1T315I. We present final results of a phase-1 vamotinib dose-escalation study to identify maximum tolerated dose (MTD) and dose-limiting toxicity (DLT) followed by expansion cohorts. 51 subjects with chronic myeloid leukaemia (CML) failing ≥ 1 2nd generation TKI or with BCR::ABL1T315I were ...
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Окнина Л. Б., Подлепич В. В., Sieber I. et al., Физиология человека 2026 Т. 52 № 3 С. 5–15
The aim of this study was to evaluate the frequency following response (FFR) for the analysis of the intact perception of syllables in humans. For this purpose, event-related potentials (ERPs) in response to isolated Russian syllables were recorded and analyzed in 29 healthy persons in two frequency ranges, standard (1-40 Hz) and high frequency (70-150 ...
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Sukhorukov G., Paramonov A., Lisak O. et al., PLoS Neglected Tropical Diseases 2023 Vol. 17 No. 3 Article e0011141
Tick-borne encephalitis virus (TBEV) is a flavivirus which causes an acute or sometimes chronic infection that frequently has severe neurological consequences, and is a major public health threat in Eurasia. TBEV is genetically classified into three distinct subtypes; however, at least one group of isolates, the Baikal subtype, also referred to as "886-84-like", challenges this ...
Added: April 8, 2023
Slesarchuk N., Khvatov E., Chistov A. et al., Bioorganic and Medicinal Chemistry Letters 2020 Vol. 30 No. 10 Article 127100
Rigid amphipathic fusion inhibitors are potent broad-spectrum antivirals based on the perylene scaffold, usually decorated with a hydrophylic group linked via ethynyl or triazole. We have sequentially simplified these structures by removing sugar moiety, then converting uridine to aniline, then moving to perylenylthiophenecarboxilic acids and to perylenylcarboxylic acid. All these polyaromatic compounds, as well as ...
Added: March 17, 2020
Vladimir A. Korshun, RSC advances 2019 Vol. 9 No. 45 P. 26014–26023
The propargylamide of N3-Pom-protected 5-(perylen-3-ylethynyl)uracil acetic acid, a universal precursor, was used in a CuAAC click reaction for the synthesis of several derivatives, including three ramified molecules with high activities against tick-borne encephalitis virus (TBEV). Pentaerythritol-based polyazides were used for the assembly of molecules containing 2/4 antiviral 5-(perylen-3-ylethynyl) uracil scaffolds, the first examples of polyvalent perylene antivirals. Cluster compounds ...
Added: November 8, 2019
Vladimir A. Korshun, European Journal of Medicinal Chemistry 2019 Vol. 171 P. 93–103
Rigid amphipathic fusion inhibitors (RAFIs) are potent antivirals based on a perylene core linked with a
nucleoside moiety. Sugar-free analogues of RAFIs, 5-(perylen-3-ylethynyl)uracil-1-acetic acid 1 and its
amides 2, were synthesized using combined protection group strategy. Compounds 1 and 2 appeared to
have low toxicity on porcine embryo kidney (PEK) or rhabdomiosarcoma (RD) cells together with
remarkable activity against ...
Added: November 8, 2019
Rigid amphipathic fusion inhibitors demonstrate antiviral activity against African swine fever virus
Vladimir A. Korshun, Journal of General Virology 2018 Vol. 99 No. 1 P. 148–156
Rigid amphipathic fusion inhibitors (RAFIs) are a family of nucleoside derivatives that inhibit the infectivity of several enveloped viruses by interacting with virion envelope lipids and inhibiting fusion between viral and cellular membranes. Here we tested the antiviral activity of two RAFIs, 5-(Perylen-3-ylethynyl)-arabino-uridine (aUY11) and 5-(Perylen-3-ylethynyl) uracil-1-acetic acid (cm1UY11) against African swine fever virus (ASFV), for which no ...
Added: November 8, 2019
Vladimir A. Korshun, Antiviral Research 2018 Vol. 149 P. 164–173
Most antivirals target viral proteins and are specific for only one virus, or viral type. Whereas viral proteins are encoded in the plastic viral genome, virion lipids are not and their rearrangements during fusion are conserved
among otherwise unrelated enveloped viruses. Antivirals that inhibit these lipid rearrangements could thus pose
a high barrier to resistance and have broad-spectrum ...
Added: November 8, 2019
Vladimir A. Korshun, Organic Preparations and Procedures International 2017 Vol. 49 No. 4 P. 377–381
Multigram scale synthesis of 5-(perylen-3-ylethynyl)-arabino-uridine (aUY11), a potent inhibitor of enveloped viruses replication, has been developed. The compound was prepared from arabino-uridine in four steps and 54% overall yield. ...
Added: November 6, 2019