EPR spin probe and biocatalytic characterization of different species of halloysite mineral

The EPR spin probe and Biocatalytic characterization of Pristine halloysite nanoclayand natural halloysite mineral originated from ore has been performed. The more positive surface charge, the higher activity of both the immobilized enzyme and intrinsic catalytic activity of Halloysite material. The highest hemicellulose activity was demonstrated by the enzyme immobilized on Halloysite surface by covalent binding with APTES. © 2019 Author(s)

EPR Spin Probe and Biocatalytic Characterization of Different Species of Halloysite Mineral

We acknowledge the financial support of the Program 211 of the Government of the Russian Federation № 02.A03.21.0006, RFBR grants 17-03-00641 and 18-29-12129mk, the State Task from the Ministry of the Education and Science of the Russian Federation № 4.9514.2017/8.9

The effect of platinum compounds on the viability of cultured malignant neoplasm cells

The aim of the study – to study the effect of cycloplatinated complexes on the viability of tumor cells and the detection of chemical compounds for the creation of new antitumor drugs.Цель исследования – изучить влияние циклоплатинированных комплексов на жизнеспособность опухолевых клеток и синтезировать химические соединения для создания новых противоопухолевых препаратов

Indolyl-Derived 4H-Imidazoles: PASE Synthesis, Molecular Docking and In Vitro Cytotoxicity Assay

The strategy of the nucleophilic substitution of hydrogen (SNH) was first applied for the metal-free C-H/C-H coupling reactions of 4H-imidazole 3-oxides with indoles. As a result, a series of novel bifunctional azaheterocyclic derivatives were obtained in yields up to 95%. In silico experiments on the molecular docking were performed to evaluate the binding possibility of the synthesized small azaheterocyclic molecules to the selected biotargets (BACE1, BChE, CK1δ, AChE) associated with the pathogenesis of neurodegenerative diseases. To assess the cytotoxicity for the synthesized compounds, a series of in vitro experiments were also carried out on healthy human embryo kidney cells (HEK-293). The leading compound bearing both 5-phenyl-4H-imidazole and 1-methyl-1H-indole moieties was defined as the prospective molecule possessing the lowest cytotoxicity (IC50 > 300 µM on HEK-293) and the highest binding energy in the protein–ligand complex (AChE, −13.57 kcal/mol). The developed compounds could be of particular interest in medicinal chemistry, particularly in the targeted design of small-molecule candidates for the treatment of neurodegenerative disorders. © 2023 by the authors.Ministry of Education and Science of the Russian Federation, Minobrnauka: 075-15-2022-1118, W03.31.0034; Russian Science Foundation, RSF: 20-73-10077The chemical design, synthesis and characterization of indolyl-derived 4H -imidazoles and in vitro studies were supported by the Russian Science Foundation (Project # 20-73-10077). The in silico studies were supported by the Ministry of Science and Higher Education of the Russian Federation (Ref. # 075-15-2022-1118, dated 29 June 2022). The synthesis of starting 4H -imidazole N -oxide substrates was supported by the Ministry of Science and Higher Education of the Russian Federation (Project # 14.W03.31.0034)

New heterocyclic compounds of the azolopyrimidine series with pronounced antitumor activity

The purpose of the study was to study the effect of new azolopyrimidine compounds on the viability of cultured tumor cells and to identify promising compounds for the development of new antitumor drugs.Цель исследования – изучение влияния новых азолопиримидиновых соединений на жизнеспособность культивируемых опухолевых клеток и выявление перспективных соединений для разработки новых противоопухолевых препаратов

CK2 Inhibition and Antitumor Activity of 4,7-Dihydro-6-nitroazolo[1,5-a]pyrimidines

Today, cancer is one of the most widespread and dangerous human diseases with a high mortality rate. Nevertheless, the search and application of new low-toxic and effective drugs, combined with the timely diagnosis of diseases, makes it possible to cure most types of tumors at an early stage. In this work, the range of new polysubstituted 4,7-dihydro-6-nitroazolo[1,5-a]pyrimidines was extended. The structure of all the obtained compounds was confirmed by the data of 1H, 13C NMR spectroscopy, IR spectroscopy, and elemental analysis. These compounds were evaluated against human recombinant CK2 using the ADP-GloTM assay. In addition, the IC50 parameters were calculated based on the results of the MTT test against glioblastoma (A-172), embryonic rhabdomyosarcoma (Rd), osteosarcoma (Hos), and human embryonic kidney (Hek-293) cells. Compounds 5f, 5h, and 5k showed a CK2 inhibitory activity close to the reference molecule (staurosporine). The most potential compound in the MTT test was 5m with an IC50 from 13 to 27 µM. Thus, our results demonstrate that 4,7-dihydro-6-nitroazolo[1,5-a]pyrimidines are promising for further investigation of their antitumor properties. © 2022 by the authors.Ministry of Education and Science of the Russian Federation, Minobrnauka: FEUZ-2020–0058, H687.42B.223/20This work was financially supported by the Ministry of Science and Higher Education of the Russian Federation, State Contract № FEUZ-2020–0058 (H687.42B.223/20)

Investigation of cytotoxic effect of new mono- and as-triazines on malignantly degenerated cells

The purpose of the study is to determinate the effectiveness of the antitumor effect of new acridone and xanthone derivatives on tumor cell lines.Цель исследования – определение эффективности противоопухолевого действия исследуемых аналогов акридонов и ксантонов на опухолевые клеточные линии

Effect of new cycloplatinated complexes on the viability of cultured human glioblastoma and osteosarcoma cells

The article presents the results of studies conducted on cell cultures of glioblastoma and osteosarcoma (lines A-172 and HOS). The effect of new platinum compounds on the viability of cultured cells was studied. As a result, a visible cytotoxic effect was observed.В статье представлены результаты исследований, которые были проведены на клеточных культурах глиобластомы и остеосаркомы (линии А-172 и HOS). Исследовалось влияние новых соединений платины на жизнеспособность культивируемых клеток. В результате был отмечен видимый цитотоксический эффек