Publications by authors named "Latocha M"

Article Synopsis
  • New acetylene derivatives of quinoline sulfonamides were synthesized through reactions with acetylene amines, leading to hybrid systems combining quinoline and 1,2,3-triazole.
  • The structures of these compounds were confirmed using advanced techniques like NMR spectroscopy and HR-MS.
  • Testing revealed that acetylene derivatives of 8-hydroxyquinoline-5-sulfonamide showed significant anticancer activity, particularly one compound that was effective against multiple cancer cell lines and had low toxicity in non-cancer cells, outperforming standard treatments in some cases.
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Multidrug resistance is a serious problem in modern medicine and the reason for the failure of various therapies. A particularly important problem is the occurrence of multidrug resistance in cancer therapies which affects many cancer patients. Observations on the effect of metformin-a well-known hypoglycemic drug used in the treatment of type 2 diabetes-on cancer cells indicate the possibility of an interaction of this substance with drugs already used and, as a result, an increase in the sensitivity of cancer cells to cytostatics.

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In the presented work, a series of 22 hybrids of 8-quinolinesulfonamide and 1,4-disubstituted triazole with antiproliferative activity were designed and synthesised. The title compounds were designed using molecular modelling techniques. For this purpose, machine-learning, molecular docking, and molecular dynamics methods were used.

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Background: Materials have been distributed in the European Union to inform physicians on the safe use of intravitreal aflibercept (IVT-AFL) as part of the risk-minimization plan for IVT-AFL.

Objective: We aimed to measure physician knowledge and understanding of key safety information for IVT-AFL.

Methods: The current study was a follow-up cross-sectional survey ('wave 2') to an earlier survey ('wave 1') examining the effectiveness of the IVT-AFL educational materials by assessing physician knowledge of the key safety information.

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Following the publication of the joint The International Commissions on Radiation Units and Measurements (ICRU) and on Radiological Protection (ICRP) report on new operational quantities for radiation protection, the European Dosimetry Group (EURADOS) have carried out an initial evaluation. The EURADOS report analyses the impact that the new quantities will have on: radiation protection practice; calibration and reference fields; European and national regulation; international standards and, especially, dosemeter and instrument design. The task group included experienced scientists drawn from across the various EURADOS working groups.

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In this paper, we describe a new method for synthesizing hybrid combinations of 1,2,3-triazoles with a tetracyclic quinobenzothiazinium system. The developed approach allowed for the production of a series of new azaphenothiazine derivatives with the 1,2,3-triazole system in different positions of the benzene ring. In practice, the methodology consists of the reaction of triazole aniline derivatives with thioquinanthrenediinium -chloride.

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Cancer cells need to carefully regulate their metabolism to keep them growing and dividing under the influence of different nutrients and oxygen levels. Muscle isoform 2 of pyruvate kinase (PKM2) is a key glycolytic enzyme involved in the generation of ATP and is critical for cancer metabolism. PKM2 is expressed in many human tumors and is regulated by complex mechanisms that promote tumor growth and proliferation.

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A new method for modifying the structure of tetracyclic quinobenzothiazinium derivatives has been developed, allowing introduction of various substituents at different positions of the benzene ring. The method consists of reacting appropriate aniline derivatives with 5,12-(dimethyl)thioquinantrenediinium bis-chloride. A series of new quinobenzothiazine derivatives was obtained with propyl, allyl, propargyl and benzyl substituents in 9, 10 and 11 positions, respectively.

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Hybrids 1,4-quinone with quinoline were obtained by connecting two active structures through an oxygen atom. This strategy allows to obtain new compounds with a high biological activity and suitable bioavailability. Newly synthesized compounds were characterized by various spectroscopic methods.

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One of the hallmarks of cancer cells is aerobic glycolysis (the Warburg effect). The effect of dichloroacetate (DCA) is to switch glucose metabolism (cellular respiration) to a more efficient process involving oxygen, reduce the production of lactic acid, activate the respiratory chain, change the potential of the mitochondrial membrane, and release pro-apoptotic mediators (cytochrome c and AIF) into the cytosol. As a result, the control over the mutated cells is improved, their sensitivity to various drugs or radiotherapy and their sensitivity to apoptosis increase.

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Diabetes as chronic civilization disease, very often occurs together with health disorders. One of the basic pharmaceuticals commonly used in her therapy is metformin. Many other positive effects, not related to diabetes, have been observed in tatients treated with metformin for a long time.

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A series of new tertiary phenothiazine derivatives containing a quinoline and a pyridine fragment was synthesized by the reaction of 1-methyl-3-benzoylthio-4-butylthioquinolinium chloride with 3-aminopyridine derivatives bearing various substituents on the pyridine ring. The direction and mechanism of the cyclization reaction of intermediates with the structure of 1-methyl-4-(3-pyridyl)aminoquinolinium-3-thiolate was related to the substituents in the 2- and 4-pyridine position. The structures of the compounds were analyzed using H, C NMR (COSY, HSQC, HMBC) and X-ray analysis, respectively.

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Article Synopsis
  • Thirty diethylphosphate derivatives of betulin were synthesized and tested for cytotoxic effects against several human cancer cell lines, showing promising activity, particularly against amelanotic melanoma and glioblastoma.
  • The compounds demonstrated varying IC values, with some having strong potential to induce apoptosis, indicated by changes in specific markers like H3, TP53, BAX, and BCL-2.
  • Molecular docking studies indicated that the most active derivatives interacted significantly with the EGFR protein, with binding affinities comparable to the standard drug erlotinib, and further molecular dynamics revealed stable complexes forming after a brief duration.
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Article Synopsis
  • This research investigates the bonding of betulin derivatives to 1,4-quinone fragments using a triazole linker, highlighting their potential as effective substrates for the enzyme DT-diaphorase (NQO1).
  • The anticancer activities of these compounds were evaluated against various human cancer cell lines, revealing that effectiveness varies based on the specific 1,4-quinone structure and the levels of NQO1 in the targeted cells.
  • Additionally, molecular docking studies indicate that the 1,4-quinone moiety significantly affects the compounds' positioning within the NQO1 enzyme's active site, suggesting promising avenues for future medical applications.
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Depending on temperature, the 2-amino-2H-[1,2,3]triazolo[4,5-g]quinoline-4,9-dione forms two polymorphic structures, which differ in the spatial arrangement of the amine group. Both polymorphs were investigated using different experimental methods as well as various quantum chemical calculations in order to characterise their molecular structures. We used X-ray diffraction, FT-IR and NMR (solid-state and liquid) methods supplemented by the density functional theory (DFT) calculations, molecular electrostatic potential (MEP) and molecular orbital (HOMO, LUMO) analyses.

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A series of novel 1,2,3-triazole-diazphenothiazine hybrids was designed, synthesized, and evaluated for anticancer activity against four selected human tumor cell lines (SNB-19, Caco-2, A549, and MDA-MB231). The majority of the synthesized compounds exhibited significant potent activity against the investigated cell lines. Among them, compounds and showed excellent broad spectrum anticancer activity, with IC values ranging from 0.

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Article Synopsis
  • 10-1,9-diazaphenothiazine was created by reacting diphenylamine with elemental sulfur, and new derivatives were synthesized with different alkyl groups attached to the nitrogen atom.
  • Advanced NMR techniques and X-ray diffraction were used to confirm the structure of the compound.
  • The derivatives showed significant anticancer activity, outperforming cisplatin against several cancer cell lines, with specific compounds triggering apoptosis through the mitochondrial pathway.
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Article Synopsis
  • Betulin-1,4-quinone hybrids were created by linking two active structures, enhancing their biological activity and bioavailability.
  • The synthesized compounds were tested against various cancer cell lines (glioblastoma, melanoma, breast, and lung) and displayed significant cytotoxic effects, particularly in cells with high NQO1 protein levels.
  • Molecular docking studies revealed that the type of 1,4-quinone influenced the compounds' interaction with the NQO1 protein and the resulting increase in expression of the TP53 gene, indicating a potential mechanism for inducing apoptosis in certain cancer cells.
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We present efficient synthesis of isomeric types of angularly fused diquinothiazines in the reactions of 2,2'-dichloro-3,3'-diquinolinyl disulfide and diquinodithiin with 3-, 5-, 6- and 8-aminoquinolines. The pentacyclic diquinothiazine ring systems were identified as diquino[3,2-b;3',4'-e][1,4]thiazine, diquino[3,2-b;5',6'-e][1,4]thiazine, diquino[3,2-b;6',5'-e][1,4]thiazine and diquino[3,2-b;8',7'-e][1,4]thiazine with advanced two-dimensional H and C NMR techniques (COSY, ROESY, HSQC and HMBC) of N-methyl derivatives. The identification of pentacyclic ring system was confirmed by X-ray diffraction analysis of selected N-alkyl derivatives.

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New 10-substituted derivatives of 3,6-diazaphenothiazine, containing the triple bond linker terminated with tertiary cyclic and acyclic amine groups, were synthesized and screened for their anticancer action. The compounds exhibited varied anticancer activities against human glioblastoma SNB-19, melanoma C-32, and breast cancer MDA-MB231 cell lines, depending on the nature of the substituents. The most active 3,6-diazaphenothiazine, , was the derivative with the ,-diethylamino-2-butynyl substituent against glioblastoma SNB-19, and was ten times more potent than cisplatin.

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The CuAAC reaction of azides and acetylenic triterpenes was used for synthesis of new triazoles of 3-acetylbetulin and betulone. The triazole derivatives were evaluated for their anticancer activity in vitro against amelanotic melanoma C-32, ductal carcinoma T47D and glioblastoma SNB-19 cell lines. 28-[1-(3'-Deoxythymidine-5'-yl)-1-1,2,3-triazol-4-yl]carbonylbetulone exhibited a significant IC value (0.

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A synthesis of new 2,6-disubstituted and 2,6,8-trisubstituted 7-methylpurines as well as 8-substituted 3,7-dimethylxanthines containing a triple bond chain have been worked out. Purinethiones and xanthinethiones were converted into propynylthio derivatives, which were then further transformed via a Mannich reaction into aminobutynylthio derivatives (amine = pyrrolidine, piperidine, morpholine, and diethylamine). The products thus obtained represent various types of the purine and xanthine structure: 8-mono-, 2,6- and 6,8-dipropynylthio, 6- and 8-monoaminobutynylthio, 2,6- and 6,8-diaminobutynylthio derivatives.

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Betulin derivatives containing a 1,2,3-triazole ring possess a wide spectrum of biological activities, including antiviral, anticancer, and antibacterial activity. A series of novel triazoles were prepared by the 1,3-dipolar cycloaddition reaction between the alkyne derivatives of betulin and organic azides. The chemical structures of the obtained compounds were defined by ¹H and C NMR, IR, and high-resolution mass spectrometry (HR-MS) analysis.

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The compounds produced by a living organism are most commonly as medicinal agents and starting materials for the preparation of new semi-synthetic derivatives. One of the largest groups of natural compounds consists of products containing a 1,4-benzoquinone subunit. This fragment occurs in three enediyne antibiotics, dynemicin A, deoxydynemicin A, and uncilamicin, which exhibit high biological activity.

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In this study, a series of regioisomeric acetylenic sulfamoylquinolines are designed, synthesized, and tested in vitro for their antiproliferative activity against three human breast cacer cell lines (T47D, MCF-7, and MDA-MB-231) and a human normal fibroblast (HFF-1) by 4-[3-(4-iodophenyl)-2-(4-nitrophenyl)-2-5-tetrazolio]-1,3-benzene disulfonate (WST-1) assay. The antiproliferative activity of the tested acetylenic quinolinesulfonamides is comparable to that of cisplatin. The bioassay results demonstrate that most of the tested compounds show potent antitumor activities, and that some compounds exhibit better effects than the positive control cisplatin against various cancer cell lines.

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