Wyniki wyszukiwania dla: CANCER CELLS, CELLULAR RESPONSE, C-1748
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4-methyl-1-nitroacridine derivative C-1748 induces apoptosis, mitotic catastrophe or senescence in human colon carcinoma HCT116 cells depending on p53 status
PublikacjaPrzeprowadzone badania miały na celu określenie zdolności pochodnej 4-metylo-1-nitroakrydyny C-1748 do uruchomienia apoptozy, katastrofy mitotycznej lub procesu starzenia komórek ludzkiego raka okrężnicy HCT116 posiadających dziki gen p53 oraz podlinii nie posiadającej tego genu. Wykazano, że pochodna C-1748 indukuje apoptozę w komórkach obu linii HCT116 w sposób zależny od czasu inkubacji, przy czym komórki HCT116 p53+/+ wykazują...
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Mechanisms of Damage to DNA Labeled with Electrophilic Nucleobases Induced by Ionizing or UV Radiation
PublikacjaHypoxia—a hallmark of solid tumors—makes hypoxic cells radioresistant. On the other hand, DNA, the main target of anticancer therapy, is not sensitive to the near UV photons and hydrated electrons, one of the major products of water radiolysis under hypoxic conditions. A possible way to overcome these obstacles to the efficient radio- and photodynamic therapy of cancer is to sensitize the cellular DNA to electrons and/or ultraviolet...
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Pre-clinical toxicology and pathology of 9-(2'-hydroxyethylamino)-4-methyl-1-nitroacridine (C-1748), a novel anti-cancer agent in male Beagle dogs
PublikacjaPraca zawiera wyniki badań przedklinicznych i morfologicznych pochodnej akrydyny o symbolu C-1748 przeprowadzonych na psach. Wyznaczono maksymalną dawkę tolerowaną oraz przeprowadzono analizy zmiany składu krwi i morfologii jej komórek, pracy aminotransferaz, fosfokinaz, fosfataz i innych enzymów funkcjonalnych. Obserwowano też zachowanie się zwierząt. Stwierdzono, że związek ten wykazuje stosunkowo niską toksyczność, co przy obserwowanej...
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The II phase metabolism of endogenous and exogenous compounds, including antitumor chemotherapeutics
PublikacjaThe II phase metabolism, it is a set of metabolism and excretion pathways of endogenous as well as exogenous compounds including xenobiotics. UDP-glucuronyltransferases (UGTs; EC 2.4.1.17) are the most crucial representatives of II phase enzymes, which are responsible for the transformation of bilirubine and bile acids, steroids and thyroid hormones and lipids. Exogenous compounds, including drugs, carcinogens, environmental pollutants...
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Cytochrome P450 izoenzymes involved in metabolism of antitumor 9-amino-1-nitroacridine derivatives, C-857, C-1748
PublikacjaPraca jest częścią szerszych badań zmierzających do poznania molekularnego mechanizmu metabolicznej transformacji przeciwnowotworowych pochodnych 9-amino-1-nitroakrydyny. W naszym zespole wyselekcjonowano pochodną nowej generacji, która w porównaniu z poprzednimi wykazała znacznie obniżoną toksyczność ogólną. W wyniku przeprowadzonych badań wykazaliśmy, że nowa pochodna jest znacznie mniej podatna na metabolizm katalizowany przez...
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DNA modification by 1-nitroacridine derivatives. Comparison of 32P-Postlabeling and restriction enzyme analysis method for the detection of DNA adducts formed by 1-nitroacridines C-1748 and C-857
Publikacja4-podstawione 1-nitroakrydyny reprezentują nową grupę pochodnych akrydyny, zsyntetyzowanych na Politechnice Gdańskiej. Metoda 32P-postlabellingu wykazała, że pochodne C-1748 i C-857 tworzą od 4-6 adduktów DNA w systemie komórkowym i bezkomórkowym o innym rozkładzie plam chromatograficznych, jednakże niezależnym od zastosowanego systemu aktywacyjnego. Metoda enzymatycznej analizy restrykcyjnej pozwoliła natomiast śledzić kinetykę...
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A mechanistically approached review upon assorted cell lines stimulated by athermal electromagnetic irradiation
PublikacjaThe probable influence of electromagnetic irradiation on cancer treatment has been deduced from the interaction of artificial electromagnetic emissions with biological organisms. Nonetheless, the suspected health effects induced by electromagnetic-based technology imply that such a treatment may contaminate the adjacent healthy cells. Thus, gaining mechanistic insights into the problem is required to avoid athermal health hazards....
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Successive cytotoxicity control by evolutionary surface decorated electronic push-pull green ZnCr-LDH nanostructures: Drug delivery enlargement for targeted breast cancer chemotherapy
PublikacjaThe reason for the increasing bioavailability and biocompatibility of the porous nanomaterials in the presence of different (bio)molecules is still unknown. The role of difference functional groups and their interactions with the potential bioavailability and biocompatibility is of great importance. To investigate the potential contribution of the electronic effects (especially on the surface of the porous nanomaterials) on their...
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The imidazoacridinone C-1311 induces p53-dependent senescence or p53-independent apoptosis and sensitizes cancer cells to radiation
PublikacjaC-1311 is a small molecule, which has shown promise in a number of preclinical and clinical studies. However, the biological response to C-1311 exposure is complicated and has been reported to involve a number of cell fates. Here, we investigated the molecular signaling which determines the response to C-1311 in both cancer and non-cancer cell lines. For the first time we demonstrate that the tumor suppressor, p53 plays a key role...
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Interactions between bioactive components determine antioxidant, cytotoxic and nutrigenomic activity of cocoa powder extract
PublikacjaNumerous studies have shown, rather disappointingly, that isolated bioactive phytochemicals are not as biologically effective as natural plant products. Such a discrepancy may be explained by the concept of food synergy, which was verified in this research for cocoa extract versus its major components with regard to cancer chemoprevention. The evaluation embraced the relationship between redox properties evaluated in cell-free systems...
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Naturally-derived hydrogels for 3D pancreatic tumor models: A short review
PublikacjaStatistics suggest a high proportion of mortality rate by pancreatic cancer, which is a solid tumor characterized by high heterogeneity and the presence of a complex extracellular matrix. The very low effectiveness of pancreatic cancer treatment roots in the high metastatic potential and drug resistance of this tumor. Therefore, the quest for efficient cellular models enabling precise mimicking in vivo conditions, and anticancer...
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Pregnane X receptor dependent up-regulation of CYP2C9 and CYP3A4 in tumor cells by antitumor acridine agents, C-1748 and C-1305, selectively diminished under hypoxia
PublikacjaInduction of proteins involved in drug metabolism and in drug delivery has a significant impact on drug-drug interactions and on the final therapeutic effects. Two antitumor acridine derivatives selected for present studies, C-1748 (9-(2’-hydroxyethylamino)-4-methyl-1-nitroacridine) and C-1305 (5-dimethylaminopropylamino-8-hydroxy-triazoloacridinone), expressed high and low susceptibility to metabolic transformations with liver...
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Antitumor 1-nitroacridine derivative C-1748, induces apoptosis, necrosis or senescence in human colon carcinoma HCT8 and HT29 cells.
PublikacjaC-1748 jest związkiem oddziaływującym z DNA i potencjalnym związkiem przeciwnowotworowym szczególnie wobec nowotworów prostaty i jelita grubego przeszczepialnych na myszach.W pracy badano odpowiedź komórek nowotworowych HCT8 i HT29 na działanie pochodnej C-1748, w stężeniach biologicznie istotnych (EC90). Analiza cyklu komórkowego linii HCT8 pokazała, że związek powoduje wzrost frakcji sub-G1, świadczący o apoptozie tych komórek...
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Relationship between Chemical Structure and Biological Activity Evaluated In Vitro for Six Anthocyanidins Most Commonly Occurring in Edible Plants
PublikacjaNumerous studies have provided evidence that diets rich in anthocyanins show a broad spectrum of health benefits. Anthocyanins in nature are usually found in the form of glycosides. Their aglycone forms are called anthocyanidins. The chemical structure of anthocyanins is based on the flavylium cation, but they differ in the position and number of substituents. However, the bioactives and foods that contain them are frequently treated...
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Effect of C-1748 derivatives on the biofilm formation of C. albicans ATCC 10231 cells
Dane BadawczeThe datasets contain the results of the impact of five C-1748 derivatives (IKE28 - IKE32) on the biofilm formation of Candida albicans strain ATCC 10231 cells. Photographic documentation prepared with the TECAN Spark 10M titration plate reader.
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Effect of C-1748 derivatives on the morphological transformation of C. albicans ATCC 10231 cells
Dane BadawczeThe datasets contain the results of the impact of five C-1748 derivatives (IKE28 - IKE32) on morphological transformation of Candida albicans strain ATCC 10231 cells. Photographic documentation prepared with the TECAN Spark 10M titration plate reader.
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The induction of autophagy in human colon wt p53 and p53-null HCT116 cells by 4-methyl-1-nitroacridine derivative C-1748
PublikacjaPrzeprowadzone badania miały na celu określenie zdolności pochodnej 4-metylo-1-nitroakrydyny C-1748 do uruchomienia autofagii komórek ludzkiego raka okrężnicy HCT116 posiadających dziki gen p53 oraz podlinii nie posiadającej tego genu. Wszystkie eksperymenty przeprowadzone zostały przy stężeniu hamującym proliferację komórek nowotworowych w 90%. Wykazano, że indukowana przez C-1748 autofagia w komórkach raka okrężnicy jest zależna...
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The Action Mechanisms, Anti-Cancer and Antibiotic-Modulation Potential of Vaccinium myrtillus L. Extract
PublikacjaHerbal medicinal products containing Vaccinium myrtillus L. (bilberry) fruits and fruit extracts are widely available in the market. Although bilberry leaves and stems are considered as bio-waste, they contain much higher levels of phenolic compounds than fruits. The study aimed to investigate the antimicrobial and anticancer potential of aerial part extracts from Vaccinium myrtillus L. (V. myrtillus, VM) plants harvested at high...
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Development of biocompatible iron oxide-silicon oxide core-shell nanoparticles as subcellular delivery platform for glucosamine-6-phosphate synthase inhibitors
PublikacjaIn order to develop the preparation of iron oxide-silica coreshell nanoparticles (CSNPs), thesis deeply explores the cetyltrimethylammonium (CTA+) directed silica coating methods of the oleic-acid capped iron oxide nanoparticles (OA-IONPs) initialized under near-neutral pH conditions. It is demonstrated that the initial alkaline hydrolysis of ethyl acetate in the presence of CTA+ and OA-IONPs induces an unusual ligand exchange...
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Modulation of CYP3A4 activity and induction of apoptosis, necrosis and senescence by the antitumor imidazoacridinone C-1311 in human hepatoma cells
PublikacjaThere is increasing evidence that the expression level of drug metabolic enzymes affects the final cellular response following drug treatment. Moreover, anti-tumour agents may modulate enzymatic activity and/or cellular expression of metabolic enzymes in tumour cells. We investigated the influence of CYP3A4 overexpression on the cellular response induced by the anti-tumour agent C-1311 in hepatoma cells. C-1311-mediated CYP3A4...
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Telomerase inhibition - unfulfilled hopes in the perfect molecular target
PublikacjaTelomerase plays a pivotal role in cell proliferation, homeostasis, and neoplastic transformation, making it a promising molecular target for cancer chemotherapy. Of note, although hTERT has been explored thoroughly as a target, none of the promising molecules has been approved as a drug until now. The subject of research conducted as part of my doctoral dissertation is explaining the cellular and molecular mechanism of action...
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Effect Of Resveratrol And Quercetin On Telomerase Regulation In Cancer Cells And Their Anti-Cancer Potential
PublikacjaTelomeres and telomerase are nowadays one on targets for anticancer therapy. Telomerase is expressed in ~90% of human cancer cell lines and tumor specimens, whereas its enzymatic activity is not detectable in most human somatic cells. Was found that some dietary compounds can modulate telomerase activity in cancer cells. This review summarizes the current knowledge about the effects of resveratrol and quercetin on telomerase regulation...
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Study on the Effect of Rotating Magnetic Field on Cellular Response of Mammalian Cells
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CYP3A4 overexpression enhances apoptosis induced by anticancer agent imidazoacridinone C-1311, but does not change the metabolism of C-1311 in CHO cells
PublikacjaWe examine whether CYP3A4 overexpression influences the rate and pattern of antitumor imidazoacridinone C-1311 metabolism, in relation to the impact of this overexpression on cell cycle progression and final cellular response of CHO cells following C-1311 treatment. Methods: Three CHO cell lines: CHO-WT, wild type, CHO-HR, overexpressing cytochrome P450 reductase (CPR) and CHO-HR-3A4, coexpressing CPR and CYP3A4 were applied....
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Imidazoacridinone C-1311 induces both autophagy and senescence in human lung cancer A549 cells
PublikacjaNiedrobnokomórkowy rak płuc (ang. NSCLC, non-small cell lung cancer), stanowiący blisko 80-87% wszystkich przypadków, jest najczęściej występującą formą raka płuc. Skuteczność dotychczas stosowanych chemoterapeutyków w stosunku do tej formy raka jest bardzo ograniczona dlatego poszukuje się nowych związków o lepszych właściwościach leczniczych. Imidazoakrydon C-1311 wykazuje wysoką aktywność cytotoksyczną wobec komórek niedrobnokomórkowego...
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Polysaccharide-based Nanocomposites for Biomedical Applications: A Critical Review
PublikacjaPolysaccharides (PSA) are taking specific position among biomaterials for advanced applications in medicine. Nevertheless, poor mechanical properties is known as the main drawback of PSA, which highlights need for PSA modification. Nanocomposites PSA (NPSA) are a class of biomaterials widely used as biomedical platforms, but despite their importance and worldwide use have not been reviewed. Herein we critically reviewed application...
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Development of Biocompatible Fe3O4@SiO2 Nanoparticles as Subcellular Delivery Platform for Glucosamine-6-phosphate Synthase Inhibitors
PublikacjaNumerous inhibitors of glucoseamine-6-phophate synthase (GlcN-6-P), the enzyme responsible from catalysis of the first step of metabolic pathway leading to metabolism 5’-diphospho-N-acetyl-D- glucosamine, were reported as effective agents for inhibiting the growth of various fungal pathogens. Among the reported inhibitors,...
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32P-postabeling detection of DNA adducts formed by 4-methyl-1-nitro-9-aminoacridine C-1748
PublikacjaWykazano zdolność do tworzenia przez nową pochodną 1-nitroakrydyny o symbolu C-1748, adduktów z DNA komórek nowotworowych oraz z DNA w systemie bezkomórkowym.
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Diamond Nanofilm Normalizes Proliferation and Metabolism in Liver Cancer Cells
PublikacjaPurpose: Surgical resection of hepatocellular carcinoma can be associated with recurrence resulting from the degeneration of residual volume of the liver. The objective was to assess the possibility of using a biocompatible nanofilm, made of a colloid of diamond nanoparticles (nfND), to fill the side after tumour resection and optimize its contact with proliferating liver cells, minimizing their cancerous transformation. Methods:...
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DNA adduct formation by C-1748, a potent antitumor 4-methyl-1-nitroacridine of lowered toxicity.
Publikacja4-podstawione 1-nitroakrydyny reprezentują nową grupę pochodnych zsyntetyzowanych na Politechnice Gdańskiej. W porównaniu do macierzystych 1-nitroakrydyn związki te wykazują obniżoną toksyczność i podwyższoną aktywność przeciwnowotworową. Wiodąca pochodna 4-metylo-1-nitroakrydyna o symbolu C-1748 jest obecnie w przygotowaniu do I fazy badań klinicznych w leczeniu raka okrężnicy. Wprowadzenie elektrodonorowej grupy metylowej w...
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Growth inhibition of cultured cancer cells by Ribes nigrum leaf extract
PublikacjaThe present article includes data on the possible selective cytotoxic effect of extract of Ribes nigrum L. growing at high Armenian landscape. For this purpose, different non-cancer (microglial BV-2 wild type (Wt), acyl-CoA oxidase 1 (ACOX1) deficient (Acox1-/-) and cancer (human colon adenocarcinoma HT29 and human breast cancer MCF7) cell lines were applied. R. nigrum leaf ethanol extract showed a growth inhibition effect towards...
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Caffeine Inhibits Differentiation Of Lung Cancer Stem Cells By Modulating Their Respiratory Metabolism
PublikacjaIt is ell established that many tumor types contain a fraction of cells, with stem cell-like properties, called cancer stem cells (CSCs), that are resistant to apoptosis induced by therapeutic agents. The presence of CSCs may explain why a standard anticancer treatment, that eliminates only differentiated cancer cells, does not lead to cancer cure.We previously showed the existence of caffeine-sensitive mechanism that controls...
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Quinoline-based thiazolyl-hydrazones target cancer cells through autophagy inhibition
PublikacjaHeterocyclic pharmacophores such as thiazole and quinoline rings have a significant role in medicinal chemistry. They are considered privileged structures since they constitute several Food and Drug Administration (FDA)-approved drugs for cancer treatment. Herein, we report the synthesis, in silico evaluation of the ADMET profiles, and in vitro investigation of the anticancer activity of a series of novel thiazolyl-hydrazones based...
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Chemical Aspects of Biological Activity of Isothiocyanates and Indoles, the Products of Glucosinolate Decomposition
PublikacjaThere is growing evidence that cancer chemoprevention employing natural, bioactive compounds may halt or at least slow down the different stages of carcinogenesis. A particularly advantageous effect is attributed to derivatives of sulfur-organic phytochemicals, such as glucosinolates (GLs) synthesized mainly in Brassicaceae plant family. GLs are hydrolysed enzymatically to bioactive isothiocyanates (ITC) and indoles, which exhibit strong...
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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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Glutathione-mediated conjugation of anticancer drugs: an overview of reaction mechanisms and biological significance for drug detoxification and bioactivation.
PublikacjaThe effectiveness of many anticancer drugs depends on the creation of specific metabolites that may alter their therapeutic or toxic properties. One significant route of biotransformation is a conjugation of electrophilic compounds with reduced glutathione, which can be non-enzymatic and/or catalyzed by glutathione-dependent enzymes. Glutathione usually combines with anticancer drugs and/or their metabolites to form more polar...
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H2AX phosphorylation, its role in DNA damage response and cancer therapy
PublikacjaDouble-strand breaks (DSBs) are the most deleterious DNA lesions, which, if left unrepaired, may have severe consequences for cell survival, as they lead to chromosome aberrations, genomic instability, or cell death. Various physical, chemical, and biological factors are involved in DSB induction. Cells respond to DNA damage by activating the so-called DNA damage response (DDR), a complex molecular mechanism developed to detect...
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The antitumor derivative, C-1748, affects CYP3A4: crosstalk between drug metabolism, CYP3A4 expression and enzymatic activity
PublikacjaJedną z głównych przeszkód w przewidywaniu wyników terapii u pacjentów z nowotworem jest indywidualny przebieg metabolizmu stosowanych leków wynikający z polimorfizmu genów enzymów metabolizujących, jak również duża zmienność farmakokinetyki leków obserwowana u różnych pacjentów podczas trwania chemioterapii. Z powodu tzw. ''wąskiego okna terapeutycznego'' występującego w przypadku terapii lekami przeciwnowotworowymi, małe zmiany...
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Combined anticancer therapy with imidazoacridinone analogue C‐1305 and paclitaxel in human lung and colon cancer xenografts—Modulation of tumour angiogenesis
PublikacjaThe acridanone derivative 5-dimethylaminopropylamino- 8- hydroxytriazoloacridinone (C-1305) has been described as a potent inhibitor of cancer cell growth. Its mechanism of action in in vitro conditions was attributed, among others, to its ability to bind and stabilize the microtubule network and subsequently exhibit its tumour- suppressive effects in synergy with paclitaxel (PTX). Therefore, the objective of the present study...
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The time-dependent cellular uptake of C−2028, CD−C−2028, QDgreen−C−2028, and QDgreen−CD−FA−C−2028 conjugates at IC80 value to normal PNT1A cells
Dane BadawczeThe time-dependent (1, 24, 48, and 72 h) cellular uptake of C−2028, CD−C−2028, QDgreen−C−2028, and QDgreen−CD−FA−C−2028 conjugates at IC80 value to normal PNT1A cells performed by Confocal Laser Scanning Microscopy (63× magnification; ZEISS LSM T-PMT, Magdeburg, Germany). Based on the fluorescence properties of these compounds, green and orange fluorescence...
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Regulated Assembly of LPS, Its Structural Alterations and Cellular Response to LPS Defects
PublikacjaDistinguishing feature of the outer membrane (OM) of Gram-negative bacteria is its asymmetry due to the presence of lipopolysaccharide (LPS) in the outer leaflet of the OM and phospholipids in the inner leaflet. Recent studies have revealed the existence of regulatory controls that ensure a balanced biosynthesis of LPS and phospholipids, both of which are essential for bacterial viability. LPS provides the essential permeability...
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The time-dependent cellular uptake of C−2028, CD−C−2028, QDgreen−C−2028, and QDgreen−CD−FA−C−2028 conjugates at IC80 value to normal MRC-5 cells
Dane BadawczeThe time-dependent (1, 24, 48, and 72 h) cellular uptake of C−2028, CD−C−2028, QDgreen−C−2028, and QDgreen−CD−FA−C−2028 conjugates at IC80 value to normal MRC-5 cells performed by Confocal Laser Scanning Microscopy (63× magnification; ZEISS LSM T-PMT, Magdeburg, Germany). Based on the fluorescence properties of these compounds, green and orange fluorescence...
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Morphological and cellular alternations of HepG2 cells overexpressing CYP3A4 after treatment with antitumor imidazoacridinone derivative C-1311
PublikacjaW pracy badano odpowiedź biologiczną komórek nowotworu wątroby HepG2 z nadekspresją izoenzymu CYP3A4 pod wpływem pochodnej imidazoakrydonu C-1311. Wyniki porównywano z odpowiedzią komórek HepG2 z tzw. wektorem zerowym.Izoeznym CYP3A4 jest jednym z izoenzymów cytochromu P450 odpowiedzialnych za przemiany metaboliczne pochodnej C-1311. Wykazano, że pochodna C-1311 indukuje w obu liniach komórkowych blok w fazie G2/M cyklu komórkowego,...
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Role of size scale of ZnO nanoparticles and microparticles on toxicity toward bacteria and osteoblast cancer cells
PublikacjaThe specific role of size scale, surface capping, and aspect ratio of zinc oxide (ZnO) particles on toxicity toward prokaryotic and eukaryotic cells was investigated. ZnO nano and microparticles of controlled size and mor- phology were synthesized by wet chemical methods. Cytotoxicity toward mammalian cells was studied using a human osteoblast cancer cell line and antibacterial activity using Gram-negative bacteria (Escherichia...
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Cytotoxicity of C-2028, QDgreen-FA, QDred-FA, QDgreen-FA-C-2028 and QDred-FA-C-2028 aginst H460 cancer cells
Dane BadawczeThis study presents absorbance values of formazan product (converted from MTT) which corresponds the cytotoxicity of C-2028, QDgreen-FA, QDred-FA, QDgreen-FA-C-2028 and QDred-FA-C-2028 aginst H460 cancer cells. FA (folic acid) was used as a linker between quantum dots (QDs) and compound (C-2028) at different concentration (50-200 µM).
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Diminished toxicity of C-1748, 4-methyl-9-hydroxyethylamino-1-nitroacridine, compared with its demethyl analog, C-857, corresponds to its resistance to metabolism in HepG2 cells
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Glutathione conjugation of the antitumor-active 1-nitroacridine derivatives compounds C-857 and C-1748 – the major role of glutathione S-transferase M1-1
Dane BadawczeObjectives: C-857 and C-1748 are antitumor-active agents, monomers of unsymmetrical bisacridine derivatives. The aim of this study was to analyze their glutathione (GSH) conjugation in vitro in the presence of glutathione S-transferase (GST) M1-1.
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Differential Response of MDA-MB-231 and MCF-7 Breast Cancer Cells to In Vitro Inhibition with CTLA-4 and PD-1 through Cancer-Immune Cells Modified Interactions
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Exploring the Antitumor Efficacy of N-Heterocyclic Nitrilotriacetate Oxidovanadium(IV) Salts on Prostate and Breast Cancer Cells
PublikacjaThe crystal structures of two newly synthesized nitrilotriacetate oxidovanadium(IV) salts, namely [QH][VO(nta)(H2O)](H2O)2 (I) and [(acr)H][VO(nta)(H2O)](H2O)2 (II), were determined. Additionally, the cytotoxic effects of four N-heterocyclic nitrilotriacetate oxidovanadium(IV) salts— 1,10-phenanthrolinium, [(phen)H][VO(nta)(H2O)](H2O)0.5 (III), 2,2′-bipyridinium [(bpy)H][VO(nta)(H2O)](H2O) (IV), and two newly synthesized compounds...
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Targeting of FLT3-ITD kinase contributes to high selectivity of imidazoacridinone C-1311 against FLT3-activated leukemia cells
PublikacjaDrugs targeting receptor tyrosine kinase FLT3 are of particular interest since activating FLT3-internal tandem duplication (ITD) mutations abundantly occur in fatal acute myeloid leukemias (AMLs). Imidazoacridinone C-1311, a DNA-reactive inhibitor of topoisomerase II, has been previously shown to be a potent and selective inhibitor of recombinant FLT3. Here, we expand those findings by studying its effect on leukemia cells with...