Персона:
Штиль, Александр Альбертович

Организационные подразделения

Организационная единица

Институт интеллектуальных кибернетических систем

Цель ИИКС и стратегия развития - это подготовка кадров, способных противостоять современным угрозам и вызовам, обладающих знаниями и компетенциями в области кибернетики, информационной и финансовой безопасности для решения задач разработки базового программного обеспечения, повышения защищенности критически важных информационных систем и противодействия отмыванию денег, полученных преступным путем, и финансированию терроризма.

Фамилия

Штиль

Имя

Александр Альбертович

Полная страница элемента

Результаты поиска

Теперь показываю 1 - 9 из 9

Только метаданные
Conjugates of titanocene with non-steroidal anti-inflammatory drugs: synthesis, unusual NMR characteristics, stability and cytotoxicity
(2023) Guk, D. A.; Gibadullina, K. R.; Moiseeva, A. A.; Grishin, Y. K.; Shtil, A. A.; Штиль, Александр Альбертович
Только метаданные
Therapy-Induced Tumor Cell Senescence: Mechanisms and Circumvention
(2023) Zamkova, M. A.; Persiyantseva, N. A.; Tatarskiy, V. V.; Shtil, A. A.; Штиль, Александр Альбертович
Только метаданные
(4Z,4′Z)-2,2′-(Ethane-1,2-diylbis(sulfanediyl))bis(1-phenyl)-4-(pyridin-2-ylmethylene)-1H-imidazol-5(4H)-one)dicopper(II) Tetrabromide
(2023) Al-Khazraji, A. S. H.; Berezina, A. V.; Bai, X.; Tafeenko, V. A.; Shtil, A. A.; Штиль, Александр Альбертович
Только метаданные
Diethyl 2-Cyano-3-oxosuccinate
(2023) Markov, O. N.; Moiseev, A. E.; Tarasevich, B. N.; Tafeenko, V. A.; Shtil, A. A.; Штиль, Александр Альбертович
Открытый доступ
New Titanocene (IV) Dicarboxylates with Potential Cytotoxicity: Synthesis, Structure, Stability and Electrochemistry
(2023) Guk, D. A.; Gibadullina, K. R.; Burlutskiy, R. O.; Pavlov, K. G.; Shtil, A. A.; Штиль, Александр Альбертович
The search for new anticancer drugs based on biogenic metals, which have weaker side effects compared to platinum-based drugs, remains an urgent task in medicinal chemistry. Titanocene dichloride, a coordination compound of fully biocompatible titanium, has failed in pre-clinical trials but continues to attract the attention of researchers as a structural framework for the development of new cytotoxic compounds. In this study, a series of titanocene (IV) carboxylate complexes, both new and those known from the literature, was synthesized, and their structures were confirmed by a complex of physicochemical methods and X-ray diffraction analysis (including one previously unknown structure based on perfluorinated benzoic acid). The comprehensive comparison of three approaches for the synthesis of titanocene derivatives known from the literature (the nucleophilic substitution of chloride anions of titanocene dichloride with sodium and silver salts of carboxylic acids as well as the reaction of dimethyltitanocene with carboxylic acids themselves) made it possible to optimize these methods to obtain higher yields of individual target compounds, generalize the advantages and disadvantages of these techniques, and determine the substrate frames of each method. The redox potentials of all obtained titanocene derivatives were determined by cyclic voltammetry. The relationship between the structure of ligands, the reduction potentials of titanocene (IV), and their relative stability in redox processes, as obtained in this work, can be used for the design and synthesis of new effective cytotoxic titanocene complexes. The study of the stability of the carboxylate-containing derivatives of titanocene obtained in the work in aqueous media showed that they were more resistant to hydrolysis than titanocene dichloride. Preliminary tests of the cytotoxicity of the synthesised titanocene dicarboxilates on MCF7 and MCF7-10A cell lines demonstrated an IC50 в‰Ґ 100 ОјM for all the obtained compounds.
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Verubulin (Azixa) Analogues with Increased Saturation: Synthesis, SAR and Encapsulation in Biocompatible Nanocontainers Based on Ca2+ or Mg2+ Cross-Linked Alginate
(2023) Sedenkova, K. N.; Leschukov, D. N.; Grishin, Y. K.; Zefirov, N. A.; Shtil, A. A.; Штиль, Александр Альбертович
Tubulin-targeting agents attract undiminished attention as promising compounds for the design of anti-cancer drugs. Verubulin is a potent tubulin polymerization inhibitor, binding to colchicine-binding sites. In the present work, a series of verubulin analogues containing a cyclohexane or cycloheptane ring 1,2-annulated with pyrimidine moiety and various substituents in positions 2 and 4 of pyrimidine were obtained and their cytotoxicity towards cancer and non-cancerous cell lines was estimated. The investigated compounds revealed activity against various cancer cell lines with IC50 down to 1вЂ“4 nM. According to fluorescent microscopy data, compounds that showed cytotoxicity in the MTT test disrupt the normal cytoskeleton of the cell in a pattern similar to that for combretastatin A-4. The hit compound (N-(4-methoxyphenyl)-N,2-dimethyl-5,6,7,8-tetrahydroquinazolin-4-amine) was encapsulated in biocompatible nanocontainers based on Ca2+ or Mg2+ cross-linked alginate and it was demonstrated that its cytotoxic activity was preserved after encapsulation.
Открытый доступ
Imidazole-4-N-acetamide Derivatives as a Novel Scaffold for Selective Targeting of Cyclin Dependent Kinases
(2023) Rusina, P.; Gandalipov, E.; Abdusheva, Y.; Panova, M.; Shtil, A.; Штиль, Александр Альбертович
The rational design of cyclin-dependent protein kinase (CDK) inhibitors presumes the development of approaches for accurate prediction of selectivity and the activity of small molecular weight anticancer drug candidates. Aiming at attenuation of general toxicity of low selectivity compounds, we herein explored the new chemotype of imidazole-4-N-acetamide substituted derivatives of the pan-CDK inhibitor PHA-793887. Newly synthesized compounds 1-4 containing an aliphatic methyl group or aromatic radicals at the periphery of the scaffold were analyzed for the prediction of relative free energies of binding to CDK1, -2, -5, and -9 using a protocol based on non-equilibrium (NEQ) thermodynamics. This methodology allows for the demonstration of a good correlation between the calculated parameters of interaction of 1-4 with individual targets and the values of inhibitory potencies in in vitro kinase assays. We provide evidence in support of NEQ thermodynamics as a time sparing, precise, and productive approach for generating chemical inhibitors of clinically relevant anticancer targets.
Открытый доступ
Perfluorocarbon Nanoemulsions with Fluorous Chlorin-Type Photosensitizers for Antitumor Photodynamic Therapy in Hypoxia
(2023) Nguyen, M. T.; Guseva, E. V.; Ataeva, A. N.; Sigan, A. L.; Shtil, A. A.; Штиль, Александр Альбертович
The efficacy of photodynamic therapy (PDT) strictly depends on the availability of molecular oxygen to trigger the light-induced generation of reactive species. Fluorocarbons have an increased ability to dissolve oxygen and are attractive tools for gas delivery. We synthesized three fluorous derivatives of chlorin with peripheral polyfluoroalkyl substituents. These compounds were used as precursors for preparing nanoemulsions with perfluorodecalin as an oxygen depot. Therefore, our formulations contained hydrophobic photosensitizers capable of absorbing monochromatic light in the long wavelength region and the oxygen carrier. These modifications did not alter the photosensitizing characteristics of chlorin such as the generation of singlet oxygen, the major cytocidal species in PDT. Emulsions readily entered HCT116 colon carcinoma cells and accumulated largely in mitochondria. Illumination of cells loaded with emulsions rapidly caused peroxidation of lipids and the loss of the plasma membrane integrity (photonecrosis). Most importantly, in PDT settings, emulsions potently sensitized cells cultured under prolonged (8 weeks) hypoxia as well as cells after oxygen depletion with sodium sulfite (acute hypoxia). The photodamaging potency of emulsions in hypoxia was significantly more pronounced compared to emulsion-free counterparts. Considering a negligible dark cytotoxicity, our materials emerge as efficient and biocompatible instruments for PDT-assisted eradication of hypoxic cells.
Только метаданные
Biscarbocyanine dye for fluorescence imaging: Binding with albumin and DNA, cell accumulation, intracellular distribution and molecular modeling
(2023) Kostyukov, A. A.; Mestergazi, M. G.; Egorov, A. E.; Shtil, A. A.; Штиль, Александр Альбертович