Search results for "Oxazole"

showing 7 items of 227 documents

Targeting HSP90 with the small molecule inhibitor AUY922 (luminespib) as a treatment strategy against hepatocellular carcinoma

2018

Hepatocellular carcinoma (HCC) is a highly malignant tumor that responds very poorly to existing therapies, most probably due to its extraordinary inter- and intra-tumor molecular heterogeneity. The modest therapeutic response to molecular targeted agents underlines the need for new therapeutic approaches for HCC. In our study, we took advantage of well-characterized human HCC cell lines, differing in transcriptomic subtypes, DNA mutation and amplification alterations, reflecting the heterogeneity of primary HCCs, to provide a preclinical evaluation of the specific heat shock protein 90 (HSP90) inhibitor AUY922 (luminespib). Indeed, HSP90 is highly expressed in different tumor types, but it…

p53MaleCancer ResearchCellTranscriptome0302 clinical medicineHCCbeta CateninAged 80 and overLuminespibAUY922Liver NeoplasmsHep G2 CellsSorafenibMiddle AgedUp-RegulationGene Expression Regulation Neoplasticmedicine.anatomical_structureOncologyCaspases030220 oncology & carcinogenesisHepatocellular carcinomaFemaleNUPR1medicine.drugAdultSorafenibCarcinoma Hepatocellularβ-CateninMice NudeAntineoplastic AgentsSmall Molecule Libraries03 medical and health sciencesDownregulation and upregulationIn vivoCell Line TumormedicineHSP90AnimalsHumansHSP90 Heat-Shock ProteinsAgedCell growthbusiness.industryMcl-1IsoxazolesResorcinolsHCCSmedicine.diseasedigestive system diseasesMutationCancer researchTranscriptomebusinessInternational Journal of Cancer
researchProduct

Naturally Occurring Oxazole Structural Units as Ligands of Vanadium Catalysts for Ethylene-Norbornene (Co)polymerization

2021

1,3-Oxazole and 4,5-dihydro-1,3-oxazole are common structural motifs in naturally occurring peptides. A series of vanadium complexes were synthesized using VCl3(THF)3 and methyl substituted (4,5-dihydro-1,3-oxazol-2-yl)-1,3-oxazoles as ligands and analyzed using NMR and MS methods. The complexes were found to be active catalysts both in ethylene polymerization and ethylene-norbornene copolymerization. The position of methyl substituent in the ligand has considerable impact on the performance of (co)polymerization reaction, as well as on the microstructure, and thus physical properties of the obtained copolymers.

polyethyleneEthyleneSubstituentVanadiumchemistry.chemical_elementTP1-1185010402 general chemistry01 natural sciencesCatalysisCatalysischemistry.chemical_compoundPolymer chemistryCopolymervanadium catalystPhysical and Theoretical ChemistryQD1-999polyethylene; norbornene copolymers; oxazole ligand; vanadium catalyNorborneneOxazole010405 organic chemistryChemical technology0104 chemical sciencesChemistrychemistryPolymerizationnorbornene copolymersoxazole ligandCatalysts
researchProduct

Titanium and Vanadium Catalysts with 2-Hydroxyphenyloxazoline and Oxazine Ligands for Ethylene-Norbornene (co)Polymerization

2019

A series of titanium and vanadium complexes with oxazoline 2-(4,5-dihydro-1,3-oxazol-2-yl)phenol (L1), 2-(4-methyl-4,5-dihydro-1,3-oxazol-2-yl)phenol (L2), and oxazine 2-(5,6-dihydro-4H-1,3-oxazin-2-yl)phenol (L3) ligands were synthesized, and their structures were determined by NMR and MS methods as (L)2MtCl2. The vanadium complexes were found to be highly active in ethylene (7300 kgPE/(molV&middot

polyethyleneEthyleneoxazine ligandVanadiumchemistry.chemical_elementPolyethyleneCatalysisCatalysischemistry.chemical_compoundchemistryPolymerizationnorbornene copolymersPolymer chemistryCopolymervanadium catalystMolar mass distributionPhysical and Theoretical Chemistryoxazole ligandNorborneneCatalysts
researchProduct

Determination of glyphosate and its metabolite aminomethylphosphonic acid in fruit juices using supported-liquid membrane preconcentration method wit…

2005

Abstract The application of supported-liquid membrane (SLM) technique for effective extraction of N -(phosphonomethyl)glycine (glyphosate) and its primary metabolite aminomethylphosphonic acid (AMPA) from juices (orange, grapefruit, apple and blackcurrant) in combination with HPLC-UV detection after derivatization with p -toluenesulphonyl chloride (TsCl) is presented. The influence of various parameters such as the composition of acceptor phase, flow-rate, concentration of analytes, on the performance of extraction procedure, was studied. It was shown that by appropriate manipulation of SLM parameters the level of detection could be significantly improved. The influence of SLM conditions on…

supported-liquid membrane extractionMetaboliteGlycineOrganophosphonatesTetrazolesaminomethylphosphonic acidfruit juiceBiochemistryHigh-performance liquid chromatographyChlorideAnalytical ChemistryBeveragesTosyl Compoundschemistry.chemical_compoundglyphosatemedicineSample preparationAminomethylphosphonic acidDerivatizationChromatography High Pressure LiquidChromatographyOrganic ChemistryPrimary metaboliteMembranes ArtificialIsoxazolespesticidesGeneral MedicinechemistryFruitGlyphosateCalibrationSpectrophotometry UltravioletHPLCmedicine.drugJournal of Chromatography A
researchProduct

MTOR inhibitor-based combination therapies for pancreatic cancer

2018

Background: Although the mechanistic target of rapamycin (MTOR) kinase, included in the mTORC1 and mTORC2 signalling hubs, has been demonstrated to be active in a significant fraction of patients with pancreatic ductal adenocarcinoma (PDAC), the value of the kinase as a therapeutic target needs further clarification. Methods: We used Mtor floxed mice to analyse the function of the kinase in context of the pancreas at the genetic level. Using a dual-recombinase system, which is based on the flippase-FRT (Flp-FRT) and Cre-loxP recombination technologies, we generated a novel cellular model, allowing the genetic analysis of MTOR functions in tumour maintenance. Cross-species validation and pha…

therapeutic resistance0301 basic medicineCancer ResearchCell SurvivalMAP Kinase Signaling Systempancreatic cancerAntineoplastic AgentsContext (language use)Mechanistic Target of Rapamycin Complex 2mTORC1Mechanistic Target of Rapamycin Complex 1BiologymTORC2BortezomibMice03 medical and health sciencesCell Line TumorPancreatic cancermedicineAnimalsHumansExtracellular Signal-Regulated MAP KinasesMechanistic target of rapamycinPI3K/AKT/mTOR pathwayBenzoxazolesKinaseMTORTOR Serine-Threonine Kinasesmedicine.diseaseddc:3. Good healthPancreatic NeoplasmsPyrimidines030104 developmental biologyOncologybiology.proteinCancer researchCamptothecinTOR Serine-Threonine KinasesPhosphatidylinositol 3-KinaseTranslational TherapeuticsProto-Oncogene Proteins c-aktBiologieCarcinoma Pancreatic Ductal
researchProduct

Double copies of blaKPC-3::Tn4401a on an IncX3 plasmid in Klebsiella pneumoniae successful clone ST512 from Italy

2015

ABSTRACT A carbapenem-resistant sequence type 512 (ST512) Klebsiella pneumoniae carbapenemase 3 (KPC-3)-producing K. pneumoniae strain showing a novel variant plasmid content was isolated in Palermo, Italy, in 2014. ST512 is a worldwide successful clone associated with the spread of bla KPC genes located on the IncFIIk pKpQIL plasmid. In our ST512 strain, the bla KPC-3 gene was unusually located on an IncX3 plasmid, whose complete sequence was determined. Two copies of bla KPC-3 ::Tn 4401a caused by intramolecular transposition events were detected in the plasmid.

transposonsequence analysispolymerase chain reactionDrug ResistanceGene DosageSettore MED/42 - Igiene Generale E Applicatabacterial proteinbeta-Lactamaseopen reading framecarbapenemasePlasmidminocyclineplasmid DNAmeropenemPharmacology (medical)geneticscolistincefpodoximeceftazidime610 Medicine & healthCarbapenemBacterialpolymyxin Btimentingene expression regulationbacteriumKlebsiella pneumoniae carbapenemase 3 producing Klebsiella pneumoniae3. Good healthantiinfective agentmicrobial sensitivity testKlebsiella pneumoniaeItalypriority journaltigecyclineMultipleclone (Java method)cefotaxime030106 microbiologyKlebsiella pneumoniae carbapenemase 3tobramycinMicrobial Sensitivity Testsgentamicinpiperacillin plus tazobactamchemistryGene dosageArticleMicrobiology03 medical and health sciencesComplete sequenceClone CellOpen Reading FramesertapenemBacterial Proteinsmultidrug resistanceextensively drug resistant bacteriumAnti-Bacterial AgentcefepimePharmacologylevofloxacinmicrobiologycefoxitinbiochemical phenomena metabolism and nutritionbacterial infections and mycosesVirologyAnti-Bacterial Agents; Bacterial Proteins; Carbapenems; Clone Cells; Drug Resistance Multiple Bacterial; Gene Dosage; Italy; Klebsiella Infections; Klebsiella pneumoniae; Microbial Sensitivity Tests; Open Reading Frames; Plasmids; beta-Lactamases; DNA Transposable Elements; Gene Expression Regulation Bacterial; Pharmacology (medical); Pharmacology; Infectious Diseasesantibiotic sensitivityClone CellsKlebsiella InfectionsceftriaxoneCarbapenemsbacterial genetics0301 basic medicinemolecular cloningSettore MED/07 - Microbiologia E Microbiologia ClinicaKlebsiella pneumoniaeTransposition (music)Drug Resistance Multiple Bacterialpolycyclic compoundsgenetic screeningcell clonecarbapenem derivativeKlebsiella infectionunclassified drugAnti-Bacterial AgentsInfectious Diseasesbacterial genePlasmidsenzymologydoripenemBiologyminimum inhibitory concentrationbeta-Lactamasesbeta lactamaseMechanisms of ResistanceciprofloxacinAmikacin; aztreonam; carbapenemase; cefepime; cefotaxime; cefoxitin; cefpodoxime; ceftazidime; ceftriaxone; ciprofloxacin; colistin; cotrimoxazole; doripenem; doxycycline; ertapenem; gentamicin; imipenem; Klebsiella pneumoniae carbapenemase 3; levofloxacin; meropenem; minocycline; piperacillin plus tazobactam; plasmid DNA; polymyxin B; tigecycline; timentin; tobramycin; unclassified drug; antiinfective agent; bacterial protein; beta lactamase; carbapenem derivative; transposon antibiotic sensitivity; Article; bacterial gene; bacterial genetics; bacterial strain; bacterium; bacterium detection; bacterium isolation; Escherichia coli; extensively drug resistant bacterium; gene dosage; genetic screening; Italy; Klebsiella pneumoniae; Klebsiella pneumoniae carbapenemase 3 producing Klebsiella pneumoniae; minimum inhibitory concentration; molecular cloning; nonhuman; polymerase chain reaction; priority journal; sequence analysis; cell clone; chemistry; drug effects; enzymology; gene expression regulation; genetics; isolation and purification; Klebsiella infection; Klebsiella pneumoniae; metabolism; microbial sensitivity test; microbiology; multidrug resistance; open reading frame; plasmid; transposon Anti-Bacterial Agents; Bacterial Proteins; beta-Lactamases; Carbapenems; Clone Cells; DNA Transposable Elements; Drug Resistance Multiple Bacterial; Gene Dosage; Gene Expression Regulation Bacterial; Italy; Klebsiella Infections; Klebsiella pneumoniae; Microbial Sensitivity Tests; Open Reading Frames; Plasmidsplasmidbacterium isolationEscherichia coliGeneAmikacinbacterium detectionnonhumandoxycyclineisolation and purificationGene Expression Regulation Bacterialbiology.organism_classificationbacterial straincotrimoxazoleOpen reading frameDNA Transposable Elementdrug effectsDNA Transposable Elementsmetabolismaztreonamimipenem
researchProduct

Organocatalytic Enantioselective Vinylogous Henry Reaction of 3,5-Dimethyl-4-nitroisoxazole with Trifluoromethyl Ketones

2017

The enantioselective vinylogous Henry reaction of 3,5-dimethyl-4-nitroisoxazole with trifluoromethyl ketones employing a bifunctional squaramide organocatalyst has been developed. A series of isoxazole bearing trifluoromethyl-substituted tertiary alcohols, 2-substituted (R)-1,1,1-trifluoro-3-(3-methyl-4-nitroisoxazol-5-yl)propan-2-ols, were obtained under these mild reaction conditions in good yields and moderate to good enantioselectivities

trifluoromethyl ketoneReaction conditionsNitroaldol reactionTrifluoromethyl010405 organic chemistryasymmetric synthesisisoxazoleOrganic ChemistryEnantioselective synthesisSquaramide010402 general chemistry01 natural sciencesCatalysis0104 chemical scienceschemistry.chemical_compoundchemistrysquaramide organocatalystvinylogous Henry reactionOrganic chemistryIsoxazoleBifunctionalTertiary alcoholsSynthesis
researchProduct