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Your search keyword '"Domracheva, I."' showing total 179 results
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179 results on '"Domracheva, I."'

1. Aromatic sulphonamides of aziridine-2-carboxylic acid derivatives as novel PDIA1 and PDIA3 inhibitors.

Author

Zelencova-Gopejenko, D., Andrianov, V., Domracheva, I., Kanepe-Lapsa, I., Milczarek, M., Stojak, M., Przyborowski, K., Fedak, F. A., Walczak, M., Kramkowski, K., Wietrzyk, J., Chlopicki, S., and Kalvins, I.

Subjects
ACID derivatives, PROTEIN disulfide isomerase, FIBRINOLYTIC agents, SULFONAMIDES, NUCLEAR magnetic resonance, AZIRIDINATION, AMIDES
Abstract

In this study, we report a series of newly synthesised sulphonamides of aziridine-2-carboxylic acid (Az-COOH) ester and amide analogues as potent protein disulphide isomerase (PDI, EC 5.3.4.1) inhibitors. The inhibitory activity on PDI was determined against recombinant human PDIA1 and PDIA3 proteins using an insulin reduction assay. These compounds in low micromolar to low nanomolar concentrations showed the effective in vitro inhibitory properties of PDIA1 with weaker effects on PDIA3. Complexes of 15N- and 15N,13C- uniformly labelled recombinant human PDIA1a with two PDIA1 inhibitors were produced and investigated by a protein nuclear magnetic resonance (NMR) spectroscopy. It was found that both C53 and C56 of the PDIA1 enzyme were involved in covalent binding. Finally, in a range of pharmacological studies, we demonstrated that investigated compounds displayed anti-cancer and anti-thrombotic activity. These findings demonstrate that sulphonamides of Az-COOH derivatives are promising candidates for the development of novel anti-cancer and anti-thrombotic agents. [ABSTRACT FROM AUTHOR]

Published
2023
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28. Synthesis of New Aziridine and Azetidine Derivatives as Potential MMP-2 Inhibitors

Author

Suta, K, Stamberga, D, Solops, A, Domracheva, I, and Turks, M

Subjects
RuAAC, MMP inhibitors, CuAAC
Abstract

Matrix metalloproteinases (MMPs) are zinc-dependent endopeptidases that are responsible for cleavage of extracellular matrix proteins. Because of their effect on both physiological and pathological processes, MMPs, especially MMP-2, have become interesting targets for treatment of cancer. Herein we report potency of MMP-2 inhibition among aziridine and azetidine derivatives containing 1,4- or 1,5- disubstituted triazoles in the side chain.

Published
2016

29. Search for New MMP-2 Inhibitors Among Small Nitrogen Heterocycles Containing Disubstituted 1,2,3-Triazole in the Side Chain

Author

Suta, K, Stamberga, D, Solops, A, Domracheva, I, Shestakova, I, and Turks, M

Subjects
MMP-2 inhibitors, aziridine-triazole conjugates, azide-alkyne cycloaddtition, azetidine-triazole conjugates
Abstract

Matrix metalloproteinases (MMPs) are zinc-dependent endopeptidases that are responsible for cleavage of extracellular matrix proteins such as collagen, gelatin, elastin and casein. Because of their effect on both physiological and pathological processes, MMPs have become interesting targets for treatment of cancer. In addition, it is known that MMP-2 has the most important impact to tumour growth. Previously, our research group has identified aziridine derivatives with 1,4-disubstituted 1,2,3-triazole in the side chain as a new class of MMP-2 inhibitors.2,3 Herein we report futher investigation of these aziridine derivatives as well as new research among aziridines containing 1,5-disubstituted 1,2,3-triazole and azetidines containing 1,4-disubstituted 1,2,3-triazole in the side chain.

Published
2015

30. Synthesis and MMP-2 Inhibition Studies of Novel Aziridine and Azetidine Derivatives

Author

Suta, K, Stamberga, D, Solops, A, Domracheva, I, Shestakova, I, Stepanovs, D, and Turks, M

Subjects
MMP-2 inhibitors, aziridine-triazole conjugates, azetidine-triazole conjugates
Abstract

Matrix metalloproteinases (MMPs) are zinc-dependent endopeptidases that are responsible for cleavage of extracellular matrix proteins. Because of their effect on both physiological and pathological processes, MMPs have become interesting targets for treatment of cancer. In addition, it is known that MMP-2 has the most important impact to tumor growth. Based on previous research, new series of aziridine and azetidine derivatives containing 1,4-disubstituted 1,2,3-triazole in the side chain as well as aziridine derivatives containing 1,5-disubstituted 1,2,3-triazole in the side chain were synthesized using transition metals catalyzed Huisgen 1,3-dipolar cycloaddition. MMP-2 inhibition studies of target compounds revealed some promising results among aziridine derivatives containing 1,4-disubstituted 1,2,3-triazole, while for other two series inhibition potency was not detected.

Published
2015

31. Synthesis and Evaluation of Reducing Capacity and Calcium Channel Blocking Activity of Novel 3,5-Dipropargylcarbonyl-Substituted 1,4-Dihydropyridines*

Author

Rucins, M., primary, Gosteva, M., additional, Domracheva, I., additional, Kanepe-Lapsa, I., additional, Belyakov, S., additional, Plotniece, M., additional, Pajuste, K., additional, Cekavicus, B., additional, Jekabsone, M., additional, Sobolev, A., additional, Shestakova, I., additional, and Plotniece, А., additional

Published
2014
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41. Method based on atomic photoionization for spot-size measurement on focused soft x-ray free-electron laser beams

Author

Sorokin, A. A., primary, Gottwald, A., additional, Hoehl, A., additional, Kroth, U., additional, Schöppe, H., additional, Ulm, G., additional, Richter, M., additional, Bobashev, S. V., additional, Domracheva, I. V., additional, Smirnov, D. N., additional, Tiedtke, K., additional, Düsterer, S., additional, Feldhaus, J., additional, Hahn, U., additional, Jastrow, U., additional, Kuhlmann, M., additional, Nunez, T., additional, Plönjes, E., additional, and Treusch, R., additional

Published
2006
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50. Styrylpyridinium Derivatives for Fluorescent Cell Imaging.

Author

Putralis R, Korotkaja K, Kaukulis M, Rudevica Z, Jansons J, Nilova O, Rucins M, Krasnova L, Domracheva I, Plotniece M, Pajuste K, Sobolev A, Rumnieks F, Bekere L, Zajakina A, Plotniece A, and Duburs G

Abstract

A set of styrylpyridinium (SP) compounds was synthesised in order to study their spectroscopic and cell labelling properties. The compounds comprised different electron donating parts (julolidine, p -dimethylaminophenyl, p -methoxyphenyl, 3,4,5-trimethoxyphenyl), conjugated linkers (vinyl, divinyl), and an electron-withdrawing N -alkylpyridinium part. Geminal or bis -compounds incorporating two styrylpyridinium ( bis -SP) moieties at the 1,3-trimethylene unit were synthesised. Compounds comprising a divinyl linker and powerful electron-donating julolidine donor parts possessed intensive fluorescence in the near-infrared region (maximum at ~760 nm). The compounds had rather high cytotoxicity towards the cancerous cell lines HT-1080 and MH-22A; at the same time, basal cytotoxicity towards the NIH3T3 fibroblast cell line ranged from toxic to harmful. SP compound 6e had IC 50 values of 1.0 ± 0.03 µg/mL to the cell line HT-1080 and 0.4 µg/mL to MH-22A; however, the basal toxicity LD 50 was 477 mg/kg (harmful). The compounds showed large Stokes' shifts, including 195 nm for 6a , b , 240 nm for 6e , and 325 and 352 nm for 6d and 6c , respectively. The highest photoluminescence quantum yield (PLQY) values were observed for 6a , b , which were 15.1 and 12.2%, respectively. The PLQY values for the SP derivatives 6d , e (those with a julolidinyl moiety) were 0.5 and 0.7%, respectively. Cell staining with compound 6e revealed a strong fluorescent signal localised in the cell cytoplasm, whereas the cell nuclei were not stained. SP compound 6e possessed self-assembling properties and formed liposomes with an average diameter of 118 nm. The obtained novel data on near-infrared fluorescent probes could be useful for the development of biocompatible dyes for biomedical applications.

Published
2023
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