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Wyniki wyszukiwania dla: ANTIPROLIFERATIVE ACTIVITY
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New conjugates of mycophenolic acid and their antiproliferative activity
PublikacjaThe new conjugates of mycophenolic acid (MPA) were obtained in the reaction of N6-(ω-aminoalkyl)adenosines with MPA in the presence of EDCI as a coupling reagent. New compounds 4a–h were evaluated on leukemia cell line (Jurkat) and PBMC from healthy donors. Length of the linker influenced observed activity. The compound 4b possessing 1,3-diamine spacer exhibited the most promising results and can be considered to further investigations.
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Synthesis and antiproliferative activity of new mycophenolic acid conjugates with adenosine derivatives
PublikacjaNew conjugates of mycophenolic acid (MPA) and adenosine derivatives were synthesized and assessed as potential immunosuppressants on Jurkat cell line and peripheral blood mononuclear cells (PBMC) from healthy donors. As compared to MPA, all compounds were found to be more active against Jurkat cell line. The antiproliferative activities were compared with MPA and adenosine, in both 2′,3′-O-isopropylidene protected and free hydroxyl...
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Synthesis of Usnic Acid Derivatives and Evaluation of Their Antiproliferative Activity against Cancer Cells
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Structure–bioavailability relationship study of genistein derivatives with antiproliferative activity on human cancer cell
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Synthesis and antiproliferative activity of conjugates of adenosine with muramyl dipeptide and nor-muramyl dipeptide derivatives
PublikacjaWe synthesized a series of MDP(D,D) and nor-MDP(D,D) derivatives conjugated with adenosine through a spacer as potential immunosuppressants. New conjugates were evaluated on two leukemia cell lines (Jurkat and L1210) and PBMC from healthy donors.
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Antiproliferative Activity of Double Point Modified Analogs of 1,25-Dihydroxyvitamin D2 Against Human Malignant Melanoma Cell Lines
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Antiproliferative activity of side-chain truncated vitamin D analogs (PRI-1203 and PRI-1204) against human malignant melanoma cell lines
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Modification of Rapana thomasiana hemocyanin with choline amino acid salts significantly enhances its antiproliferative activity against MCF-7 human breast cancer cells
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Thermodynamic, Anticoagulant, and Antiproliferative Properties of Thrombin Binding Aptamer Containing Novel UNA Derivative
PublikacjaThrombin is a serine protease that plays a crucial role in hemostasis, fibrinolysis, cell proliferation, and migration. Thrombin binding aptamer (TBA) is able to inhibit the activity of thrombin molecule via binding to its exosite I. This 15-nt DNA oligonucleotide forms an intramolecular, antiparallel G-quadruplex structure with a chair-like conformation. In this paper, we report on our investigations on the influence of certain...
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Organic and conventional kiwifruit, myths versus reality: antioxidant, antiproliferative and helth effects
PublikacjaComparison between organic and conventional kiwifruit cultivars 'Hayward' and 'Bidan', which was done by four radical scavenging assays, ESI-MS, and DSC measurements, showed significant differences between the cultivars. Such results were not estimated in kiwifruit growing under organic and conventional conditions. The extraction of bioactive compounds was done by two different methods: sequential extraction with ethyl acetate...
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Antimicrobial and Antiproliferative Coatings for Stents in Veterinary Medicine—State of the Art and Perspectives
PublikacjaMicrobial colonization in veterinary stents poses a significant and concerning issue in veterinary medicine. Over time, these pathogens, particularly bacteria, can colonize the stent surfaces, leading to various complications. Two weeks following the stent insertion procedure, the colonization becomes observable, with the aggressiveness of bacterial growth directly correlating with the duration of stent placement. Such microbial...
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Organic and conventional kiwifruit myths versus reality: antioxidant, antiproliferative and health effects
PublikacjaComparison between organic and conventional kiwifruit cultivars ''Hayward'' and ''Bidan'', which was done by four redical scavenging assays, ESI-MS, and DSC measurements, showed significant differences between cultivars. Such results were not estimated in kiwifruit growing under organic and conventional conditions. The extraction of bioactive compounds was done by two different methods: sequential extraction with ethyl acetate...
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A comparative study of phenolic compounds and antioxidant and antiproliferative activities in frequently consumed raw vegetables
PublikacjaCelem badań było oszacowanie właściwości przeciwutleniających wybranych warzyw spożywczych w stanie surowym: czosnek (Allium sativum L), biała, żółta i czerwona cebula (Allium cepa L), czerwony i zielony pieprz (Capsicum annuum L.) oraz biała kapusta (Brassica oleracea var. capitata f. alba) zbieranych w ciągu tego samego roku z różnych regionów geograficznych i stref klimatycznych. W badaniach odpowiednich ekstraktów metanolowych...
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Comparison of bioactive compounds, antioxidant and antiproliferative activities of Mon Thong durian during ripening
PublikacjaCelem przeprowadzonych badań było oszacowanie zmian zawartości związków odżywczych, związków bioaktywnych, kwasów tłuszczowych oraz przeciwutleniaczy w owocach duriana w trakcie różnych etapów procesu dojrzewania. W badaniach wykorzystano testy CURRAC, DPPH, ABTS i FRAP. Stwierdzono, że całkowita zawartość polifenoli, flawonoidów, kwasu askorbimowego, tanin oraz poziom aktywności przeciwutleniającej jest dla owoców niedojrzałych,...
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Tetrahydroquinolinone derivatives exert antiproliferative effect on lung cancer cells through apoptosis induction
PublikacjaThe anticancer properties of quinolones is a topic of interest among researchers in the scientific world. Because these compounds do not cause side effects, unlike the commonly used cytostatics, they are considered a promising source of new anticancer drugs. In this work, we designed a brief synthetic pathway and obtained a series of novel 8-phenyltetrahydroquinolinone derivatives functionalized with benzyl-type moieties at position...
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Phenolic compounds from Nerium oleander leaves: microwave assisted extraction, characterization, antiproliferative and cytotoxic activities
PublikacjaA microwave-assisted extraction (MAE) method was used for the extraction of phenolic compounds from Nerium oleander leaves. The influence of variables such as ethanol concentration, microwave power, irradiation time and liquid/solid ratio on polyphenol extraction was modelled using a second-order regression equation based on response surface methodology (RSM). The optimal conditions for MAE were: extraction solvent 35% ethanol...
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Design, synthesis, and biological evaluation of tetrahydroquinolinones and tetrahydroquinolines with anticancer activity
PublikacjaColorectal cancer (CRC) is the most commonly diagnosed cancer in Europe and the United States and the second leading cause of cancer related mortality. A therapeutic strategy used for the treatment of CRC involves targeting the intracellular levels of reactive oxygen species (ROS). In this study, we synthesized a series of novel tetrahydroquinolinones and assessed their ability to inhibit CRC growth and proliferation by evoking...
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The comparison of cytotoxic and genotoxic activities of glucosinolates, isothiocyanates, and indoles
PublikacjaChemopreventive properties of Brassica vegetables are attributed mainly to their characteristic compounds—glucosinolates (GLs) and their main hydrolysis products—isothiocyanates (ITCs) and indoles. In this study, we compared antiproliferative activity (MTT test in HT29 cells) and genotoxic effects (comet assay in HT29 cells and restriction analysis in a cell-free system) of three GLs (sinigrin (SIN), glucotropaeolin (GTL), and...
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Palindromic carbazole derivatives: unveiling their antiproliferative effect via topoisomerase II catalytic inhibition and apoptosis induction
PublikacjaHuman DNA topoisomerases are essential for crucial cellular processes, including DNA replication, transcription, chromatin condensation, and maintenance of its structure. One of the significant strategies employed in cancer treatment involves the inhibition of a specific type of topoisomerase, known as topoisomerase II (Topo II). Carbazole derivatives, recognised for their varied biological activities, have recently become a significant...
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Novel amides of mycophenolic acid and some heterocyclic derivatives as immunosuppressive agents
PublikacjaThe group of new amide derivatives of mycophenolic acid (MPA) and selected heterocyclic amines was synthesised as potential immunosuppressive agents functioning as inosine-5'-monophosphate dehydrogenase (IMPDH) uncompetitive inhibitors. The synthesis employed uronium-type activating system (TBTU/HOBt/DIPEA) while or phosphonic acid anhydride method (T3P/Py) facilitating amides to be obtained in moderate to excellent yields without...