Search results for "Cytotoxicity"

showing 10 items of 865 documents

ChemInform Abstract: (a)-Anellated Carbazoles with Antitumor Activity: Synthesis and Cytotoxicity.

2010

The cycloadducts3,5, and7, readily available from methoxy-substituted 3-vinylindoles1 and2, were dehydrogenated withDDQ to the coplanar [a]-anellated carbazoles4,6, and8. Compound4a, also characterized by X-ray structural analysis, shows significant cytotoxicity against K562 und RXF393 human tumor cell lines.

Antitumor activityHuman tumorStereochemistryCell cultureChemistryGeneral MedicineCytotoxicityK562 cellsChemInform
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Oxygenated Cembrene Diterpenes from Sarcophyton convolutum: Cytotoxic Sarcoconvolutum A–E

2021

The soft coral genus Sarcophyton contains the enzymatic machinery to synthesize a multitude of cembrene-type diterpenes. Herein, highly oxygenated cembrenoids, sarcoconvolutum A–E (1–5) were purified and characterized from an ethyl acetate extract of the red sea soft coral, Sarcophyton convolutum. Compounds were assemblies according to spectroscopic methods including FTIR, 1D- and 2D-NMR as well as HRMS. Metabolite cytotoxicity was tested against lung adenocarcinoma, cervical cancer, and oral-cavity carcinoma (A549, HeLa and HSC-2, respectively). The most cytotoxic compound, (4) was observed to be active against cell lines A549 and HSC-2 with IC50 values of 49.70 and 53.17 μM, respectively.

Aquatic Organismssarcoconvolutum A–EMagnetic Resonance Spectroscopy<i>Sarcophyton convolutum</i>StereochemistryQH301-705.5MetaboliteEthyl acetatePharmaceutical ScienceAntineoplastic AgentsArticleHeLaInhibitory Concentration 50Structure-Activity Relationshipchemistry.chemical_compoundCell Line TumorDrug DiscoveryIc50 valuesAnimalsCytotoxic T cellBiology (General)CytotoxicityIndian OceanPharmacology Toxicology and Pharmaceutics (miscellaneous)cembrenoidschemistry.chemical_classificationbiologyChemistrySarcophyton<i>Sarcophyton convolutum</i>; sarcoconvolutum A–E; cembrenoids; cytotoxicitySarcophyton convolutumAnthozoabiology.organism_classificationEnzymecytotoxicityDiterpenesDrug Screening Assays AntitumorMarine Drugs
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New organotin(IV) complexes with L-Arginine,Nα-t-Boc-L-Arginine and L-Alanyl-L-Arginine.Synthesis, structural investigations and cytotoxic activity

2010

Abstract Novel diorganotin(IV) derivatives of l -Arginine (HArg), N α -( tert -Butoxycarbonyl)- l -Arginine (Boc–Arg–OH) and l -Ala- l -Arg (H 2 Ala–Arg), H 2 NC( NH)NH(CH 2 ) 3 CH(NHR′)CO 2 H, where R′ = H in HArg, R′ = C(O)OC(CH 3 ) 3 in Boc–Arg–OH, R′ = H 2 NCH(CH 3 )CO in H 2 Ala–Arg and triorganotin(IV) derivatives of Boc–Arg–OH have been synthesized and structurally characterized. The complexes were investigated by FT-IR and 119 Sn Mossbauer in the solid state and by 1 H, 13 C, 119 Sn and 1 H– 1 H COSY NMR spectroscopy, in solution. The spectroscopic characterization leading to the proposed molecular structures was accomplished on the basis of these experiments. l -Arginine appears to…

ArginineStereochemistryLigandOrganic ChemistryL-Arginine; Boc-Arg-OH; L-Alanyl-L-Arginine; organotin(IV); NMR; cytotoxic activitySubstrate (chemistry)Biological activityorganotin(IV)BiochemistryL-ArginineNMRInorganic ChemistryL-Alanyl-L-Argininechemistry.chemical_compoundchemistryBoc-Arg-OHSettore CHIM/03 - Chimica Generale E InorganicaMaterials ChemistryChelationCarboxylatePhysical and Theoretical ChemistryCytotoxicityTwo-dimensional nuclear magnetic resonance spectroscopycytotoxic activity
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Folate-targeted supramolecular vesicular aggregates based on polyaspartyl-hydrazide copolymers for the selective delivery of antitumoral drugs.

2010

Supramolecular vesicular aggregates (SVAs) have the advantage of combining the safe and biocompatible properties of colloidal vesicular carriers based on phospholipids with those of polymeric materials, i.e. polyaspartyl-hydrazide (PAHy) copolymers. To provide SVAs with a certain tumour selectivity, folate moieties were chemically conjugated to PAHy copolymers. Physicochemical properties (mean sizes, polydispersity index and zeta potential) of folate-targeted SVAs (FT-SVAs) loaded with gemcitabine were evaluated. The antiproliferative and anticancer activity of gemcitabine-loaded FT-SVAs was evaluated against two cancer cell lines, i.e. MCF-7 cells which over-express the folate receptor and…

AzidesMaterials sciencePolymersBiophysicsBioengineeringAntineoplastic AgentsBiocompatible MaterialsPharmacologyDeoxycytidineFlow cytometryBiomaterialsDrug Delivery SystemsFolic AcidIn vivoCell Line TumorMaterials TestingmedicineHumansTissue DistributionCytotoxicityLiposomeDrug CarriersMicroscopy Confocalmedicine.diagnostic_testMolecular StructureGemcitabineIn vitroDRUG DELIVERY POLYASPARTYLHYDRAZIDE FOLATESettore CHIM/09 - Farmaceutico Tecnologico ApplicativoMechanics of MaterialsCell cultureFolate receptorDrug deliveryCeramics and CompositesBiophysicsPeptidesBiomaterials
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Microwave-Assisted Synthesis of New Selenazole Derivatives with Antiproliferative Activity

2013

New aryl-hydrazinyl-1,3-selenazole and aroyl-hydrazonyl-1,3-selenazoles were synthesized via Hantzsch type condensation reactions of selenosemicarbazides with α-halogenocarbonyl derivatives, under classical versus microwave heating conditions. Excellent yields and shorter reaction times were obtained under irradiation conditions. The structures of the synthesized compounds were assigned based on spectroscopic data (FT-IR, 1 H-NMR), MS and elemental analysis. Selenazole derivatives were screened for their anti-proliferative effects against two leukemia cell lines (CCRF-CEM and HL60) and three carcinoma cell lines (MDA-MB231, HCT116 and U87MG).

AzolesHL60Pharmaceutical ScienceAntineoplastic AgentsHL-60 CellsMicrowave assistedArticleLeukemia cell lineAnalytical Chemistrylcsh:QD241-441Inhibitory Concentration 50chemistry.chemical_compoundlcsh:Organic chemistryselenazole; microwave assisted synthesis; cytotoxicityCell Line TumorOrganoselenium CompoundsCarcinoma CellDrug DiscoveryHumansPhysical and Theoretical ChemistryMicrowavesCell ProliferationOrganic ChemistryselenazoleHCT116 CellsCondensation reactionCombinatorial chemistrychemistryChemistry (miscellaneous)Elemental analysisMicrowave heatingcytotoxicityMolecular Medicinemicrowave assisted synthesisMolecules
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Toward the development of metal-based synthetic nucleases: DNA binding and oxidative DNA cleavage of a mixed copper(II) complex with N-(9H-purin-6-yl…

2009

Abstract The complex [Cu(N9-ABS)(phen) 2 ]·3.6H 2 O, H 2 N9-ABS  = N -(9 H -purin-6-yl)benzenesulfonamide and phen = 1,10-phenanthroline, has been synthesized and then characterized with the aid of X-ray diffraction, analytical, and spectroscopic techniques. The geometry of Cu(II) is distorted square pyramidal with the equatorial positions occupied by three N atoms from two phenantroline molecules and one N atom from the adenine ring of the sulfonamide ligand. The interaction of the complex with DNA was studied by means of viscosity measurements and fluorescence spectroscopy. The results pointed to a classic intercalation of the complex between the DNA base pairs. The complex was found to b…

Base pairStereochemistryIntercalation (chemistry)Antineoplastic AgentsApoptosisCleavage (embryo)BiochemistryJurkat cellsInorganic ChemistryJurkat Cellschemistry.chemical_compoundOrganometallic CompoundsHumansDNA CleavageCytotoxicitySulfonamidesChemistryDNASquare pyramidal molecular geometryProto-Oncogene Proteins c-bcl-2ApoptosisCaco-2 CellsTumor Suppressor Protein p53CopperDNAPhenanthrolinesJournal of Inorganic Biochemistry
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Generation of chemotactic activity by immune complexes carrying clustered or nonclustered C&amp;42horbar; sites

1973

Sensitized cells (EA) bearing different numbers of &42horbar; sites were tested for their ability to generate chemotactic activity from C-EDTA. From the results it can be shown that: 1 the amount of chemotactic activity generated parallels the number of &42horbar; sites bound to the cell surface, 2 all &42horbar; sites clustered around a single hemolytic site are enzymatically active as far as generation of chemotactic activity is concerned, and, 3 no difference can be demonstrated with IgG or IgM antibodies

Binding SitesIgm antibodyChemotaxisImmunologyCellChemotaxisAntigen-Antibody ComplexComplement System ProteinsBiologyCytotoxicity Tests ImmunologicMolecular biologyRatsImmune systemmedicine.anatomical_structureImmunologyLeukocytesmedicineAnimalsImmunology and AllergyRabbitsEdetic AcidEuropean Journal of Immunology
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Cytotoxicity of deoxynivalenol and cytoprotection of antioxidants in Caco-2 cells

2016

BiochemistryCaco-2ChemistryGeneral MedicineToxicologyCytotoxicityCytoprotectionToxicology Letters
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Isolation and Molecular Docking of Cytotoxic Secondary Metabolites from Two Red Sea Sponges of the Genus Diacarnus

2021

BiochemistryGenusChemistryCytotoxic T cellGeneral ChemistryIsolation (microbiology)CytotoxicityChemistrySelect
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The excellent biocompatibility and negligible immune response of the titanium heterometallic MOF MUV-10

2021

The Ti-Ca heterometallic MOF MUV-10 exhibits good dispersibility in phosphate buffer and low phosphate-induced degradation in comparison to other MOF systems. It induces no cytotoxicity towards cells of the immune system and no inmune response, making it an attractive candidate for biomedical applications and demonstrating its safe use for other applications.

BiocompatibilityBiomedical Engineeringchemistry.chemical_elementBiocompatible Materials02 engineering and technology010402 general chemistry01 natural sciencesMiceImmune systemMaterials TestingAnimalsHumansGeneral Materials ScienceParticle SizeCytotoxicityMetal-Organic FrameworksTitaniumfungiPhosphate buffered salineImmunityGeneral ChemistryGeneral Medicine021001 nanoscience & nanotechnologyCombinatorial chemistry0104 chemical scienceschemistryDegradation (geology)Calcium0210 nano-technologyTitaniumJournal of Materials Chemistry B
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