Radiation monitoring system

Book of Abstracts, Journal Year: 2021, Volume and Issue: unknown

Published: Jan. 1, 2021

Anna A. Oleshkevich, Specific features of change in enzymate activity

Language: Английский

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TLD-100 post-irradiation fading characteristics according to IEC 62387:2020 standard

Book of Abstracts, Journal Year: 2021, Volume and Issue: unknown

Published: Jan. 1, 2021

Anna A. Oleshkevich, Specific features of change in enzymate activity

Language: Английский

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Autophagy Modulators in Cancer Therapy

International Journal of Molecular Sciences, Journal Year: 2021, Volume and Issue: 22(11), P. 5804 - 5804

Published: May 28, 2021

Autophagy is a process of self-degradation that plays an important role in removing damaged proteins, organelles or cellular fragments from the cell. Under stressful conditions such as hypoxia, nutrient deficiency chemotherapy, this can also become strategy for cell survival. be nonselective selective specific organelles, ribosomes, and protein aggregates, although complete mechanisms regulate aspects autophagy are not fully understood. This review summarizes most recent research into understanding different types autophagy. The relationship between apoptosis on level molecular regulation expression selected proteins p53, Bcl-2/Beclin 1, p62, Atg caspases was discussed. Intensive studies have revealed whole range novel compounds with anticancer activity inhibit activate regulatory pathways involved We focused presentation strongly affecting process, particular emphasis those undergoing clinical preclinical cancer research. Moreover, target points, adverse effects therapeutic schemes inhibitors activators presented.

Language: Английский

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New 1,3,4-Thiadiazole Derivatives with Anticancer Activity

Molecules, Journal Year: 2022, Volume and Issue: 27(6), P. 1814 - 1814

Published: March 10, 2022

We designed and synthesized the 1,3,4-thiadiazole derivatives differing in structure of substituents C2 C5 positions. The cytotoxic activity obtained compounds was then determined biological studies using MCF-7 MDA-MB-231 breast cancer cells normal cell line (fibroblasts). results showed that both lines, strongest anti-proliferative exerted by 2-(2-trifluorometylophenylamino)-5-(3-methoxyphenyl)-1,3,4-thiadiazole. IC50 values this compound against were 49.6 µM 53.4 µM, respectively. Importantly, all new had weaker on than lines. In silico demonstrated a possible multitarget mode action for compounds. most likely mechanism is connected with activities Caspase 3 8 activation BAX proteins.

Language: Английский

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Preparation of Novel Pyrazolo[4,3-e]tetrazolo[1,5-b][1,2,4]triazine Sulfonamides and Their Experimental and Computational Biological Studies

International Journal of Molecular Sciences, Journal Year: 2022, Volume and Issue: 23(11), P. 5892 - 5892

Published: May 24, 2022

Pyrazolo[4,3-e]tetrazolo[1,5-b][1,2,4]triazine sulfonamides constitute a novel class of heterocyclic compounds with broad biological activity, including anticancer properties. Investigated in this study, MM-compounds (MM134, MM136, MM137, and MM139) exhibited cytotoxic proapoptotic activity against cancer cell lines (BxPC-3, PC-3, HCT-116) nanomolar concentrations without causing cytotoxicity normal cells (L929 WI38). In silico predictions indicate that tested exhibit favorable pharmacokinetic profiles may exert through the inhibition BTK kinase, AKT-mTOR pathway PD1-PD-L1 interaction. Our findings point out these sulfonamide derivatives source new drugs after optimization.

Language: Английский

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The Anticancer Action of a Novel 1,2,4-Triazine Sulfonamide Derivative in Colon Cancer Cells

Molecules, Journal Year: 2021, Volume and Issue: 26(7), P. 2045 - 2045

Published: April 2, 2021

Cancer therapy is one of the most important challenges modern medical and chemical sciences. Among many methods combating cancer, chemotherapy plays a special role. Imperfect justifies continuing search for new, more effective, safe drugs. Sulfonamides are classic group chemotherapeutic drugs with broad spectrum pharmacological activity. Recent literature reports show that sulfonamide derivatives have anti-tumor activity in vitro vivo. The aim study was to synthesize novel 1,2,4-triazine derivative check its anticancer potential DLD-1 HT-29 colon cancer cells. biological studies included MTT assay, DNA biosynthesis, cell cycle analysis, Annexin V binding ethidium bromide/acridine orange staining, caspase-8, -9, -3/7 concentrations molecules (sICAM-1, mTOR, Beclin-1, cathepsin B) involved pathogenesis poor prognosis colorectal were also evaluated by ELISA. We demonstrated compound able induce apoptosis through intrinsic extrinsic pathways capable decreasing sICAM-1, B concentrations, whereas increased Beclin-1 concentration detected both lines. represents promising multi-targeted but further vivo examinations needed confirm claim.

Language: Английский

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Exploration of novel heterofused 1,2,4-triazine derivative in colorectal cancer

Journal of Enzyme Inhibition and Medicinal Chemistry, Journal Year: 2021, Volume and Issue: 36(1), P. 535 - 548

Published: Jan. 1, 2021

Colorectal cancer (CRC) is the third leading cause of cancer-related deaths in men and women. The impact new pyrazolo[4,3-e]tetrazolo[1,5-b][1,2,4]triazine sulphonamide (MM-129) was evaluated against human colon vitro zebrafish xenografts. Our results show that this synthesised compound effectively inhibits cell survival BTK-dependent mechanism. Its effectiveness much higher at a relatively low concentration as compared with standard chemotherapy used for CRC, i.e. 5-fluorouracil (5-FU). Flow cytometry analysis after annexin V-FITC propidium iodide staining revealed apoptosis main response CRC cells to MM-129 treatment. We also found tumour development embryo xenograft model, where it showed markedly synergistic anticancer effect when combination 5-FU. above suggest novel heterofused 1,2,4-triazine derivative may be promising candidate further evaluation chemotherapeutic agent CRC.

Language: Английский

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Recent Advances in Biological Active Sulfonamide based Hybrid Compounds Part C: Multicomponent Sulfonamide Hybrids

Current Medicinal Chemistry, Journal Year: 2022, Volume and Issue: 30(37), P. 4181 - 4255

Published: Nov. 29, 2022

Sulfonamides, with the general formula R-SO2NR1R2, have attracted great attention since early discovery of sulfonamide-containing antibacterial drugs. The combinations certain sulfonamides and other drug molecules to form sulfonamide hybrids are being used develop novel formulations greater effectiveness in a huge range therapeutic applications such as antimicrobial, antifungal, anti-inflammatory, antitubercular, antiviral, antidiabetic, antiproliferative, carbonic anhydrase inhibitor, antimalarial, anticancer medicinal agents. Part C this review presents recent advances designing developing multicomponent containing more than one biologically active heterocycle, coumarin, indole, pyridine, pyrimidine, pyrazole, triazole, oxazole, oxadiazole, triazine, quinazoline, thiadiazol. This aims highlight status hybridization technique synthesizing biological computational studies that were designed presented between 2016 2020.

Language: Английский

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Novel synthesis of new triazine sulfonamides with antitumor, anti-microbial and anti-SARS-CoV-2 activities

BMC Chemistry, Journal Year: 2024, Volume and Issue: 18(1)

Published: March 26, 2024

Abstract Novel approach for synthesizing triazine sulfonamide derivatives is accomplished via reacting the sulfaguanidine with N -cyanodithioiminocarbonate. Further reaction of novel analogues various secondary amines and anilines generated substituted promising broad-spectrum activities including anti-microbial, anti-tumor, anti-viral properties. The in vitro anti-proliferative most compounds were evaluated on NCI-60 cell line panel. antifungal antibacterial also estimated. activity against SARS CoV-2 virus was performed using MTT cytotoxicity assay to evaluate half-maximal cytotoxic concentration (CC 50 ) inhibitory (IC a representative compound from category. Compound 3a demonstrated potent antiviral SARS-CoV-2 IC = 2.378 µM as compared drug remdesivir 10.11 µM). Our results indicate that, upon optimization, these new sulfonamides could potentially serve drugs.

Language: Английский

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Multi-Targeting Anticancer Activity of a New 4-Thiazolidinone Derivative with Anti-HER2 Antibodies in Human AGS Gastric Cancer Cells

International Journal of Molecular Sciences, Journal Year: 2023, Volume and Issue: 24(7), P. 6791 - 6791

Published: April 5, 2023

Combining chemotherapy with immunotherapy still remains a regimen in anticancer therapy. Novel 4-thiazolidinone-bearing hybrid molecules possess well-documented activity, and together anti-HER2 antibodies, may represent promising strategy treating patients gastric cancer confirmed human epidermal growth factor receptor 2 (HER2) expression. The aim of the study was to synthesize new 4-thiazolidinone derivative (Les-4367) investigate its molecular mechanism action combination trastuzumab or pertuzumab AGS cells. cell viability antiproliferative potential were examined. effect tested combinations as well monotherapy on apoptosis autophagy also determined. Metalloproteinase-2 (MMP-2), intercellular adhesion molecule 1 (ICAM-1), pro-inflammatory anti-inflammatory cytokine concentrations demonstrated by ELISA technique. We proved that very effective increasing sensitivity cells novel Les-4367. is connected induction apoptosis. Additionally, activity not associated process. Decreased cytokines, MMP-2 ICAM-1-were observed. drugs based antibodies Les-4367 against

Language: Английский

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