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  1. 9 Acta Biochimica Polonica
  2. 9 Wiadomości Chemiczne
  3. 4 Acta Poloniae Pharmaceutica - Drug Research
  4. 4 Bromatologia i Chemia Toksykologiczna
  5. 3 BioTechnologia. Journal of Biotechnology Computational Biology and Bionanotechnology
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  1. 1 2023
  2. 3 2022
  3. 1 2021
  4. 1 2020
  5. 3 2019
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  1. 3 Antoszczak M.
  2. 3 Huczyński A.
  3. 2 Czajkowska A.
  4. 2 Fedtchouk A. S.
  5. 2 Gogler A.
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1
Synthesis, Structure, and Pharmacological Screening of 2,7-Naphthyridine Derivatives
100%
Wagner E. , Wójcicka A. , Bryndal I. , Lis T.
Polish Journal of Chemistry
|
2009
|
tom Vol. 83, nr 2
207-215
EN
An attempt to rearrange pyrrolo[3,4-c]pyridine-1,3-diones to the 2,7-naphthyridine ring under the conditions, described in only one report [1], gave compounds 7-9, but did not yield the expected 2,7- or 2,6-naphthyridine isomers. Important for the synthesis of the naphthyridine ring from pyrrolo[3,4-c]pyridine was that, of the two possible isomers, only 2,7- not 2,6-naphthyridine was obtained. Ethyl (4-R'-1,3- dioxo- 6-phenyl-1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-yl)acetate (5, 6, 10) treated with sodium ethoxide was rearranged by the Claisen-Dieckmann reaction to ethyl 4-hydroxy-8-R'-1-oxo-6-phenyl-1,2-dihydro-2,7-naphthyridine-3-carboxylate (13, 14), where R' = methyl or ethoxy. The structures of the new compounds were confirmed by elemental analysis and NMR and IR spectra. The structure of 14 was also determined by X-ray crystallography to prove the presence of 2,7-naphthyridine isomer. The in vitro anticancer activities of the final 2,7-naphthyridines were tested at the US NCI (Bethesda, MD). Compound 13 exhibited cytostatic activity in vitro.
2
Syntheses and In Vitro Antitumor Activity of 3-Amino-N-(4-chlorobenzenesulfonyl)guanidine Derivatives Containing N'-Arylidene Moiety
100%
Sławiński J. , Bednarski P. , Reszka P.
Polish Journal of Chemistry
|
2004
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tom Vol. 78 / nr 3
369-379
EN
The syntheses of new 3-arylideneamino-1-(2-alkythio-4-chloro-5-methylbenzenesulfonyl) guanidines 2-8 and 1-arylidene-2-(2-alkylthio-4-chloro-5-R3-benzenesulfonyl)- 3-methylaminoguanidines 9-16 are described. The in vitro antitumor screening of compounds 2, 3, 9 and 10 was evaluated at the Institute of Pharmacy, University of Greifswald. The remaining compounds 5, 11-14 and 16 were screened at the National Cancer Institute (NCI) for their activities against a panel of 55 human tumor cell lines, and relationships between structure and anticancer activity in vitro are discussed. The highest anticancer activity was found for 2-(2-benzylthio-4-chloro-5-methylbenzenesulfonyl)- 3-methylamino-1-(5-nitrothienylidene)guanidine (12) (GI50 in the range 0.3-0.6 _M), while other compounds exhibit reasonable (16) or moderate ( 9, 13) anticancer activities.
3
Content available Cytotoxic and anticancer activity of Moringa oleifera
100%
Kinga Szlachetka K. , Paulina Kut P. , Agnieszka Stepien A.
European Journal of Clinical and Experimental Medicine
|
2020
|
nr 3
214-220
EN
Introduction. Given its very strong antioxidant properties, Moringa oleifera is particularly noteworthy among medicinal plants. The high contents antioxidants in the M. oleifera determining her antioxidant activities deciding for very important anticancer properties. Aim. The aim of the paper is to provide an overview of the cytotoxic and anticancer activity of Moringa oleifera. Material and methods. This review was performed based systematic analysis of literature. Analysis of the literature. The results of scientific research conducted in vitro indicate that extracts from Moringa oleifera significantly affect the development of human cancer cells such as myeloma, leukemia, cervix, breast, colon, lung, liver, neuroblastoma, pancreas, colorectal, epidermoid, oral, ovarian, muscular, prostate, skin. Conclusion. This indicates Moringa oleifera as that they may be used as a therapeutic agent to support oncological therapies.
4
Content available Synthesis, physicochemical studies, fluorescence behavior, and anticancer properties of transition metal complexes with the pyridyl ligand
100%
Azam M. , Al-Resayes S. I.
Polish Journal of Chemical Technology
|
2022
|
tom Vol. 24, nr 3
35--40
EN
A novel series of complexes with the formula [MLCl] [M = Co(II) (1), Ni(II) (2), Cu(II) (3), Zn(II) (4)] arising from Pyridyl ligand, N,N’-bis(1-(2-pyridyl)ethylidene)-2,2-dimethylpropane-1,3-diamine), ligand, L, was synthesized and investigated by elemental analyses, FT-IR, 1H and 13C NMR, Powder XRD, and thermal analyses. TGA analysis indicated that all complexes degraded in three different steps, while the PXRD examination showed well-defined sharp crystalline peaks for the complexes, indicating significant crystallinity. The antiproliferative activity of the ligand and its complexes were also evaluated in vitro against the HeLa (Human Cervical Cancer Cells) and HCT116 (Colon Cancer Cells) cell lines. The findings suggested complex 4 to be potential anticancer agent against these cell lines. In addition, ligand and its complexes also exhibited considerable emission properties.
5
Content available CHEMICAL COMPOSITION OF THE ESSENTIAL OIL AND FLAVONOIDS OF THYMUS SERPYLLUM L., GROWING ON TERRITORY OF THE EAST KAZAKHSTAN
100%
Tazabayeva K. A. , Sylibaeva B.
Acta Poloniae Pharmaceutica - Drug Research
|
2018
|
tom 75
|
nr 6
1329-1337
EN
Thymus serpyllum L. (T.serpyllum) has a great interest as a potential plant component, which is used in the production of fermented milk products with anticancer effect. The plant material was collected at the flowering stage. Chemical composition of essential oil and flavonoids from the aerial parts of the T. serpyllum, grown in the Southern Altai of the East Kazakhstan region, has been investigated for the first time. Output of the essential oil received from the aerial part of the plant in the flowering stage was on average 0,2%. Forty-one compounds were identified in T. serpyllum essential oil, which accounts for 96, 1% of the total oil. The main components of the oil were thymol (41,8%), γ-terpinene (15,3%), o-cymene (10,9%). Apart from the composition of essential oils, there were shown some flavonoids, such asapigenin 7 glucoside (0.24 % of dried plant material), luteolin (0,039 %), quercetin (0,006 %), which demonstrated a cytotoxic effect on cancer cells. In our experiments, luteolin had greater cytotoxic effect on cancer cells HCT-15 than quercetin. IC50 value of quercetin (100 μM) was higher than that of luteolin (50 μM).
6
Content available Selenium – meaning in the prevention and therapy of cancer diseases
100%
Molenda A. , Muszyńska B.
Medicina Internacia Revuo
|
2017
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tom 28
|
nr 109
272-279
EN
Selenium is a trace element supplied to the human body with food of plant and animal origin. It is a component of many enzymes with antioxidant activity, such as: glutathione peroxidase, seleniumprotein P, thioredoxin reductase and phospholipid hydroperoxide glutathione peroxidase. Being a component of enzymes, it protects cells against deformation and genetic damage thanks to the properties that inhibit the processes of lipid peroxidation, nucleic acids (DNA, RNA). The human body contains about 10-15 mg of selenium, 60% of which is found in erythrocytes, and 40% in blood. The problem of Poland and neighboring countries is the lack of this element in the soil, and therefore in the organisms of herbivorous farm animals. The lack of selenium in the meat of these animals causes significant deficiencies in the human body. In addition, due to the lack of this element in the soil, vegetables and preparations obtained from it do not constitute a suitable dietary source and intensify the problem of deficiency of this element in Europeans. Many studies indicate that both organic and inorganic selenium compounds reduce the progression of cancer by reducing the migration of cancer cells, inhibiting angiogenesis, and consequently reduce metastases.
7
Content available Synthesis and anticancer activity evaluation of some new derivatives of 2-(4-benzoyl-1-piperazinyl)-quinoline and 2-(4-cinnamoyl-1-piperazinyl)-quinoline.
100%
Kubica K. P. , Taciak P. P. , Czajkowska A. , Sztokfisz-Ignasiak A. , Wyrebiak R. , Podsadni P. , Mlynarczuk-Bialy I. , Malejczyk J. , Mazurek A. P.
Acta Poloniae Pharmaceutica - Drug Research
|
2018
|
tom 75
|
nr 4
891-901
EN
In this study we designed and synthesized twenty new derivatives of 2-(4-benzoyl-1-piperazinyl)-quinoline and 2-(4-cinnamoyl-1-piperazinyl)-quinoline with potential anticancer activity. The structures of synthesized compounds were confirmed by 1H and 13C NMR spectroscopy and MS spectrometry. The activity of novel compounds was evaluated in the cell viability assay as well as in the wound healing assay. Presented data show that examined substances have anticancer activity in cell culture. Seven compounds which showed a high rate of cell growth inhibition were selected for further studies. Three of them strongly reduced growth of B16F10 cells. The novel compounds constitute a good base for further studies and optimization of structure for new therapeutically effective anti-cancerous drugs.
8
Content available Synthesis and anticancer activity evaluation of novel derivatives of 7-amino-4-methylquinolin-2(1H)-one
100%
Kubica K. P. , Taciak P. P. , Czajkowska A. , Sztokfisz-Ignasiak A. , Wyrebiak R. , Mlynarczuk-Bialy I. , Malejczyk J. , Mazurek A. P.
Acta Poloniae Pharmaceutica - Drug Research
|
2018
|
tom 75
|
nr 4
903-910
EN
In this study we designed and synthesized sixteen new derivatives of 7-amino-4-methylquinolin-2(1H)-one with potential anticancer activity. The structures of synthesized compounds were confirmed by 1H and 13C NMR. The activity of novel substances was evaluated by cell viability assay and wound healing assay. In vitro tests for series of sixteen novel compounds were performed. The results showed that examined compounds are selective for cancer cells, but their activity for various types of cancer is different. Three of new compounds presented ability to inhibit cells migration. The novel compounds constitute a good starting point for further studies and optimization of structure for new therapeutically effective anti-cancerous drugs. Seven compounds, which showed the highest rate of cell inhibition, were selected for further studies.
9
Syntheses of N,S-Substituted 4-Chloro-2-mercapto-5-methylbenzenesulfonamide Derivatives with Potential Biological Activity
100%
Pomarnacka E. , Kornicka A. , Bednarski P. J. , Charkiewicz A.
Polish Journal of Chemistry
|
2009
|
tom Vol. 83, nr 1
65-73
EN
The syntheses of N,S-substituted 4-chloro-2-mercapto-5-methylbenzenesulfonamide derivatives are described. The compounds 6-11, 14, 15 and 19-22 were tested for their in vitro anticancer activity against 9 human cancer cell lines. The most active compounds 6, 9 and 20 showed moderate cytotoxic activity and were approximately 5-fold less potent than cisplatin.
10
Content available Design, Efficient Synthesis, Mechanism of Reaction and Antiproliferative Activity Against Cancer And Normal Cell Lines of A Novel Class of Fused Pyrimidine Derivatives
88%
roaiah h. F. , Rashdan H. R. , soliman a. , Muhammed Z. , Wietrzyk J. , Milczarek M.
Acta Poloniae Pharmaceutica - Drug Research
|
2018
|
tom 75
|
nr 3
EN
This work concentrated on the utility of hydrazonoyl halides in synthesis of bioactive heterocycles like triazoles, pyrazoles, pyrimidines and their fused derivatives which have a wide spectrum of pharmaceutical value. Herein we discussed the synthesis of new heterocyclic compounds containing fused pyrimidine rings derived from hydrazonoyl halides and their significant pharmaceutical importance as anticancer agents. New fused pyrimidine derivatives bearing 1,2,3-triazole moiety were prepared via reaction of enaminone 2 with and 6-amino-2-thioxo-pyrimidin-4-one and then with hydrazonoyl chlorides 6a-h. In addition 3-amino-6-(2-oxo-2H-chromen-3-yl)pyridine-2-carbonitrile (12) was submitted to react with carbon dioxide to afford 3-(1,2,3,4-tetrahydro-2,4-dithioxopyrido[2,3-d]pyrimidin-7-yl)-2H-chromen-2-one (15), which act as key molecule for synthesis of new series of fused prymidinethione derivatives containing coumarine moiety via its reaction with different selected derivatives of hydrazonoyl halides 6a-h. Structures of the newly synthesized compounds were confirmed using spectral data (IR, H1NMR and Mass spectrometry) and microanalytical methods. Also, they screened for their anticancer activity.
11
Content available remote A Comparison of Antioxidant, Antibacterial, and Anticancer Activity of the Selected Thyme Species by Means of Hierarchical Clustering and Principal Component Analysis
75%
Orłowska M. , Pytlakowska K. , Mrozek-Wilczkiewicz A. , Musioł R. , Waksmundzka-Hajnos M. , Sajewicz M. , Kowalska T.
Acta Chromatographica
|
2016
|
tom Vol. 28, no. 2
207--221
EN
In this study, six numerical data sets are presented valid for eighteen thyme (Thymus L.) species and characterizing three biological properties of these herbs, i.e., antioxidant, antibacterial, and anticancer activity. Four data sets characterize antioxidant properties, one data set characterizes antibacterial property, and one data set characterizes anticancer activity. Antioxidant properties were measured with two free radical standards (DPPH and ABTS), two free radical scavenger standards (trolox and gallic acid), and three analytical techniques (EPR spectroscopy, ultraviolet–visible [UV–vis] spectrophotometry, and the dot blot test with bioautographic detection). Antibacterial activity was tested upon the Gram-positive Bacillus subtilis (ATCC 6633) strain, and anticancer activity was evaluated upon the human colon adenocarcinoma cells (HCT116). It was found out that the thyme extracts characterize with all three biological activities (yet with anticancer activity not very strongly pronounced) and that in quantitative terms, each activity strongly depends on the thyme species considered. An ultimate goal of this study was to investigate if any quantitatively confirmed correlation exists among these three biological activities, which might point out to a common mechanism of their action. To this effect, six sets of numerical data underwent hierarchical clustering and Principal Component Analysis. Based on the results obtained, no quantitative correlation was established among antioxidant, antibacterial, and anticancer activity of the thyme species, which seems indicative of different molecular mechanisms of these three actions.
12
Antiproliferative activity of new benzimidazole derivatives
75%
Blaszczak-Swiatkiewicz K. , Olszewska P. , Mikiciuk-Olasik E.
Acta Biochimica Polonica
|
2013
|
tom 60
|
nr 3
EN
A series of new benzimidazole derivatives were synthesized and tested in vitro for possible anticancer activity. Their effect of proliferation into selected tumor cell lines at normoxia and hypoxia conditions was determined by WST-1 test. Additionally, apoptosis test (caspase 3/7 assay) was used to check the mode caused by the agents of cell death. Four of the examined compounds (7, 8, 13, 11) showed a very good antiproliferative effect and three of them were specific for hypoxia conditions (8, 14, 11). Compound 8 was the most cytotoxic against human lung adenocarcinoma A549 cells at hypoxic conditions. Hypoxia/ normoxia cytotoxic coefficient of compound 14 (4.75) is close to hypoxia/normoxia cytotoxic coefficient of tirapazamine (5.59) - a reference compound in our experiments and this parameter locates it between mitomycin C and 2-nitroimidazole (misonidazole). Screening test of caspase-dependent apoptosis proved that exposure to A549 cells of compounds 7-8 and 13-14 for 48 h promote apoptotic cell death. These results supplement our earlier study of the activity of new potentialy cytotoxic heterocyclic compounds against selected tumor cells.
13
Content available remote Synthetic derivatives of genistein, their properties and possible applications
75%
Rusin A. , Krawczyk Z. , Grynkiewicz G. , Gogler A. , Zawisza-Puchałka J. , Szeja W.
Acta Biochimica Polonica
|
2010
|
tom 57
|
nr 1
23-34
EN
Genistein, the principal isoflavone constituent of soybean, attracts much attention as a natural molecule with significant affinity towards targets of potential medicinal interest, but also as a food supplement or prospective chemopreventive agent. Since its physicochemical properties are considered suboptimal for drug development, much effort has been invested in designing its analogs and conjugates in hope to obtain compounds with improved efficacy and selectivity. The aim of this article is to summarize current knowledge about the properties of synthetic genistein derivatives and to discuss possible clinical application of selected novel compounds. Some basic information concerning chemical reactivity of genistein, relevant to the synthesis of its derivatives, is also presented.
14
Content available Phytochemical analysis, antioxidant and anticancer activity of Aerva javanica growing in district Karak, Khyber Pakhtunkhwa Pakistan
75%
Afzal S. , Khan S. , Iqbal M. , Akhtar A.
Acta Biologica
|
2021
|
tom 28
15
Content available Formation, characterization, and analysis of curcumin nanoformulation for evaluating its in vitro cytotoxicity
75%
Parmar N. , Mansuri A. , Trivedi K. , Ansari K. , Kumar P. , Bagban M. A. , Jhala D. , Patel A. , Chettiar S. S.
BioTechnologia. Journal of Biotechnology Computational Biology and Bionanotechnology
|
2023
|
tom 104
|
nr 3
16
Content available remote Antiproliferative activity of new benzimidazole derivatives
75%
Błaszczak-Świątkiewicz K. , Olszewska P. , Mikiciuk-Olasik E.
Acta Biochimica Polonica
|
2013
|
tom 60
|
nr 3
427-433
EN
A series of new benzimidazole derivatives were synthesized and tested in vitro for possible anticancer activity. Their effect of proliferation into selected tumor cell lines at normoxia and hypoxia conditions was determined by WST-1 test. Additionally, apoptosis test (caspase 3/7 assay) was used to check the mode caused by the agents of cell death. Four of the examined compounds (7, 8, 13, 11) showed a very good antiproliferative effect and three of them were specific for hypoxia conditions (8, 14, 11). Compound 8 was the most cytotoxic against human lung adenocarcinoma A549 cells at hypoxic conditions. Hypoxia/ normoxia cytotoxic coefficient of compound 14 (4.75) is close to hypoxia/normoxia cytotoxic coefficient of tirapazamine (5.59) - a reference compound in our experiments and this parameter locates it between mitomycin C and 2-nitroimidazole (misonidazole). Screening test of caspase-dependent apoptosis proved that exposure to A549 cells of compounds 7-8 and 13-14 for 48 h promote apoptotic cell death. These results supplement our earlier study of the activity of new potentialy cytotoxic heterocyclic compounds against selected tumor cells.
17
The analysis of structure-anticancer and antiviral activity relationships for macrocyclic pyridinophanes and their analogues on the basis of 4D QSAR models [simplex representation of molecular structure]
75%
Kuz'min V. E. , Artemenko A. G. , Lozitsky V. P. , Muratov E. N. , Fedtchouk A. S. , Dyachenko N. S. , Nosach L. N. , Gridina T. L. , Shitikova L. I. , Mudrik L. M. , Mescheriakov A. K. , Chelombitko V. A. , Zheltvay A. I. , Vanden Eynde J. J.
Acta Biochimica Polonica
|
2002
|
tom 49
|
nr 1
EN
A new 4D-QSAR approach has been considered. For all investigated molecules the 3D structural models have been created and the set of conformers (fourth dimension) have been used. Each conformer is represented as a system of different simplexes (tetratomic fragments of fixed structure, chirality and symmetry). The investigation of influence of molecular structure of macrocyclic pyridino- phanes, their analogues and certain other compounds on anticancer and antiviral (anti-influenza, antiherpes and antiadenovirus) activity has been carried out by means of the 4D-QSAR. Statistic characteristics for QSAR of PLS (partial least squares) models are satisfactory (R = 0.92-0.97; CVR = 0.63-0.83).
18
The effects of taxol [paclitaxel] on chemiluminescence of neutrophils, macrophages and J.774.2 cell line
75%
Czuba Z. P. , Krol W. , Hasinski P. , Nowowiejska A.
Acta Biochimica Polonica
|
1998
|
tom 45
|
nr 1
EN
Taxol (paclitaxel) is a chemotherapeutic diterpene with promising anticancer activity that blocks cell division by preventing microtubule depolymerization. Furthermore, recent studies have shown that taxol has other intracellular effects that may contribute to its effect, particularly in macrophages. The signal transduction mechanisms by which taxol stimulates macrophages to anticancer activity are not clear. The purpose of this study was to determine the effect of taxol on chemiluminescence (an indicator of the production of free radicals) of neutrophils, macrophages and murine macrophage J.774.2 cells. The chemiluminescence was measured in the presence of taxol andór phorbol myristate acetate (PMA) as a stimulant. Taxol stimulated chemiluminescence (without PMA) of neutrophils and macrophages but not of J.774.2 cells, and modulated chemiluminescence of the cells stimulated with PMA.
19
Analysis of the structure - anticancer activity relationship in a set of Schiff bases of macrocyclic 2,6-bis[2- and 4-formylaryloxymethyl]pyridines
75%
Kuz'min V. E. , Lozitsky V. P. , Kamalov G. L. , Lozitskaya R. N. , Zheltvay A. I. , Fedtchouk A. S. , Kryzhanovsky D. N.
Acta Biochimica Polonica
|
2000
|
tom 47
|
nr 3
EN
Quantitative estimation of the structure anticancer activity relationship in a series of macrocyclic Schiff bases of 2,6-bis(formylaryloxymethyl)pyridines was carried out by the topological approach. Correlation equations describing the relationship between the anticancer activity and structural parameters of the molecules studied and descriptors characterizing their structure were obtained on the basis of in vitro screening data. The influence of structure of the investigated substances as reflected by the parameters studied on the anticancer activity, was established.
20
Content available remote Molecular targets of [-]-epigallocatechin-3-gallate [EGCG]: specificity and interaction with membrane lipid rafts
63%
Patra S. K. , Rizzi F. , Silva A. , Rugina D. O. , Bettuzzi S.
|
|
tom 59
|
nr 9
217-235
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