Search results for "3003"

showing 10 items of 115 documents

Prognostic and predictive biomarkers for targeted therapy in NSCLC: For whom the bell tolls?

2015

Introduction: The discovery of molecular biomarkers and the advent of targeted therapies have led to a radical change in the treatment of several tumors, including NSCLC. In the last few years, the number of molecular biomarkers has rapidly increased, and a growing interest has been recently focused on their potential prognostic and predictive value in clinical settings. Areas covered: This review describes all the molecular biomarkers with prognostic and predictive value in NSCLC, including both clinically approved biomarkers, and emerging biomarkers under investigation in clinical trials. Liquid biopsy and applications of circulating biomarkers are also described. Expert opinion: The onco…

Oncologymedicine.medical_specialtyPathologyLung NeoplasmsOncogene Proteins Fusionmedicine.medical_treatmentClinical BiochemistryNSCLCprognostic biomarkersTargeted therapytissue biopsypredictive biomarkersInternal medicineCarcinoma Non-Small-Cell LungProto-Oncogene ProteinsDrug DiscoveryBiomarkers TumorMedicineHumansBiomarker discoveryLiquid biopsypredictive biomarkerprognostic biomarkerProtein Kinase InhibitorsPredictive biomarkerPharmacologyliquid biopsybusiness.industryDrug Discovery3003 Pharmaceutical Scienceliquid biopsy; NSCLC; predictive biomarkers; prognostic biomarkers; targeted therapy; tissue biopsy; Pharmacology; Clinical Biochemistry; Drug Discovery3003 Pharmaceutical ScienceProtein-Tyrosine KinasesPrognosistargeted therapyMolecular biomarkersPredictive valueClinical trialErbB ReceptorsCirculating biomarkersras Proteinsbusiness
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A methacrylic hyaluronic acid derivative for potential application in oral treatment of celiac disease.

2017

Objective: Aim of this work was the synthesis of a methacrylic hyaluronic acid (HA) derivative and the production, via photocrosslinking, of related hydrogels loaded with an endopeptidase intended for a potential oral treatment of celiac disease. Methods: The methacrylic derivative of HA was prepared through a one-pot procedure involving the reaction with ethylenediamine (EDA) and methacrylic anhydride (MA). The obtained derivative, named HA-EDA-MA, was used to prepare photocrosslinked hydrogels loaded with a prolyl endopeptidase derived from Flavobacterium meningosepticum (PEP FM) able to detoxify gliadin. Obtained hydrogels were recovered as gels or freeze-dried powders. Results: Hydrogel…

Pharmaceutical ScienceMethacrylic anhydrideprolyl endopeptidaseEthylenediamineAdministration OralEthylenediamine02 engineering and technologyMethacrylate010402 general chemistryMethacrylate01 natural sciencescomplex mixtureschemistry.chemical_compoundMiceProlyl endopeptidaseoral enzyme releaseDrug DiscoveryHyaluronic acidmedicineOrganic chemistryAnimalsHumansHyaluronic AcidPharmacologyChemistryAnimalDrug Discovery3003 Pharmaceutical ScienceOrganic ChemistrySerine Endopeptidasestechnology industry and agricultureUV irradiationHydrogels021001 nanoscience & nanotechnologyEthylenediaminesEndopeptidase0104 chemical sciencesSerine EndopeptidaseHydrogelCeliac DiseaseSelf-healing hydrogelsMethacrylates0210 nano-technologyProlyl OligopeptidasesDerivative (chemistry)Nuclear chemistrymedicine.drugHumanDrug development and industrial pharmacy
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Monocyte to lymphocyte blood ratio in tuberculosis and HIV patients: Comparative analysis, preliminary data

2017

Recent data confirmed the hypothesis suggested by historical studies that the ratio of peripheral blood monocytes to lymphocytes (M/L) is associated with the risk of tuberculosis (TB) disease. We retrospectively analyzed the electronic health records of tuberculosis and HIV-positive patients who had followed day-care programs at the AIDS Center of the University of Palermo, Italy. 261 patients were recruited and divided into 6 groups as follows: healthy control group (HCG: 47 pts), latent HIV negative infected TB group (LIG, 43 pts), active HIV negative tuberculosis (TAG: 61 pts), treated tuberculosis HIV negative (TTG: 44 pts), HIV drug-naive patients tested TST and QFT-IT-negative with ne…

PharmacologyCo-infected HIV/TBCTuberculosiDrug Discovery3003 Pharmaceutical ScienceCo-infected HIV/TBC; HIV infection; Monocyte to lymphocyte blood RATIO; Tuberculosis; Pharmacology; Drug Discovery3003 Pharmaceutical ScienceMonocyte to lymphocyte blood RATIOHIV infection
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Components from the Essential oil of Centaurea aeolica Guss. and C-diluta Aiton from Sicily, Italy

2015

Volatile components from florets, leaves and stems and branches of Centaurea aeolica Guss. harvested in Lipari, Sicily, Italy, were analysed by gas phase chomatography (GC) and gas chomatography mass spectrometry (GC-MS). The main constituents were β-eudesmol, caryophyllene oxide, ( E )-12-norcaryophyll-5-en-2-one and hexahydrofarnesylacetone in flowers, hexahydrofarnesylacetone, 2-methyloctadecane and tricosane in the leaves and hexadecanoic acid , caryophyllene oxide and β-eudesmol in the stems and branches . The analysis of the essential oil of the aerial parts of Centaurea diluta Aiton gave mainly fatty acids and derivatives, the main ones being hexadecanoic acid and (Z,Z)-9,12-octadeca…

PharmacologyDrug Discovery3003 Pharmaceutical ScienceOrganic Chemistryβ-eudesmolPlant ScienceHexahydrofarnesylacetoneβ-eudesmollcsh:QK1-989lcsh:Chemistrylcsh:QD241-441lcsh:QD1-999lcsh:Organic chemistryCaryophyllene oxideCentaurea dilutavolatile componentslcsh:BotanyVolatile componentCentaurea aeolicaGC-MSHexadecanoic acid
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Osteoporosis risk factors in HIV positive women with osteoporosis: A retrospective analysis

2017

Multifactorial risk factors such as HIV/HCV co-infection and antiretroviral therapy (ARV) have been associated with osteoporosis in HIV+ women. We retrospectively analysed which known risk factors were associated with the diagnosis of osteoporosis, according to the WHO definition, in HIV positive women who were followed-up at the AIDS Centre of the University of Palermo, Italy between January 2011 and December 2014. Twenty-one HIV+ women with osteoporosis (13 HIV+ mono-infected and 8 HIV/HCV co-infected females) who underwent dual-energy X-ray absorptiometry (DXA) and liver stiffness assessment were included in the study. No significant differences between the HIV and HIV/HCV group were fou…

PharmacologyHIV/HCV infectedAntiretroviral therapy; HIV infected; HIV/HCV infected; Osteoporosis; Osteoporosis risk factors; Pharmacology; Drug Discovery3003 Pharmaceutical ScienceDrug Discovery3003 Pharmaceutical ScienceHIV infectedOsteoporosiOsteoporosis risk factorAntiretroviral therapy
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Chemical Composition of the Essential Oil of Mentha pulegium Growing Wild in Sicily and its Activity on Microorganisms Affecting Historical Art Crafts

2017

The chemical composition of the essential oil from aerial parts of Mentha pulegium L. (Linné) collected in Sicily was evaluated by GC and GC-MS. The main components were pulegone (50.6%), piperitenone (27.8%) and menthone (6.9%). Comparison of this oil with other studied oils of different populations is discussed. The oil showed good antibacterial and antifungal activities against some microorganisms that infest historical art works.

Plant compositionMicroorganismPlant ScienceMenthone01 natural scienceslaw.inventionchemistry.chemical_compound0404 agricultural biotechnologylawMentha pulegiumPulegoneVolatile componentDrug DiscoveryBotanyPiperitenoneChemical compositionEssential oilPharmacologyLamiaceaebiologyDrug Discovery3003 Pharmaceutical Science04 agricultural and veterinary sciencesGeneral MedicineComplementary and Alternative Medicine2708 Dermatologybiology.organism_classification040401 food scienceMenthone0104 chemical sciences010404 medicinal & biomolecular chemistryComplementary and alternative medicinechemistryLamiaceaeMentha pulegiumPulegoneNatural Product Communications
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Aza-isoindolo and isoindolo-azaquinoxaline derivatives with antiproliferative activity

2015

Abstract Three new ring systems, pyrido[2′,3′:3,4]pyrrolo[1,2- a ]quinoxalines, pyrido[3′,2′:3,4]pyrrolo[1,2- a ]quinoxalines and pyrido[2′,3′:5,6]pyrazino[2,1- a ]isoindoles, were synthesized through an aza-substitution on the already active isoindolo-quinoxaline system and in particular in the position 7 or 4 of the isoindole moiety and in position 5 of the quinoxaline portion. All new compounds were screened by the National Cancer Institute (Bethesda, MD) against a panel of 60 human tumor cell lines. Biological results of the most active derivatives, with pGI 50 values between 7.09 and 7.27, confirmed the importance of the presence of methoxy substituents for biological activity. The ant…

QuinoxalineIsoindolesAzaisoindolo-quinoxalinesStereochemistryAntiproliferative activity; Apoptosis; Azaisoindolo-quinoxalines; DNA interaction; Isoindolo-azaquinoxalines; Quinoxalines; Antineoplastic Agents; Apoptosis; Aza Compounds; Cell Line Tumor; Cell Proliferation; Dose-Response Relationship Drug; Drug Screening Assays Antitumor; Humans; Isoindoles; Molecular Structure; Quinoxalines; Structure-Activity Relationship; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry; Pharmacology; Medicine (all)ApoptosisAntineoplastic AgentsAntiproliferative activityIsoindolesRing (chemistry)Drug Screening AssaysCell LineDose-Response Relationshipchemistry.chemical_compoundStructure-Activity RelationshipQuinoxalineCell Line TumorQuinoxalinesDrug DiscoverymedicineMoietyHumansAntiproliferative activity; Apoptosis; Azaisoindolo-quinoxalines; DNA interaction; Isoindolo-azaquinoxalines; Quinoxalines; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry; PharmacologyCell ProliferationPharmacologyAza CompoundsAzaisoindolo-quinoxalineTumorDose-Response Relationship DrugMolecular StructureDrug Discovery3003 Pharmaceutical ScienceMedicine (all)Organic ChemistryApoptosiBiological activityGeneral MedicineAntitumorCell cycleSettore CHIM/08 - Chimica FarmaceuticaDNA interactionSettore ING-IND/22 - Scienza E Tecnologia Dei MaterialiMechanism of actionchemistryIsoindolo-azaquinoxalineDrug Screening Assays Antitumormedicine.symptomDrugIsoindoleIsoindolo-azaquinoxalines
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Ru(bpy)2Cl2: A catalyst able to shift the course of the photorearrangement in the Boulton-Katritzky reaction

2015

The Boulton-Katritzky reaction represents one of the most popular and efficient strategies used to realize azole-into-azole conversions. For example, under different experimental conditions, it allows the rearrangement of Z-arylhydrazones of 3-benzoyl-5-phenyl-1,2,4-oxadiazoles (1) into 2-aryl-4-benzoylamino-5-phenyl-2H-1,2,3-triazoles (2) in very high yields. Moreover, we have recently realized this conversion also by UV-photostimulation. Now we have enlarged the scope of the reaction irradiating with visible or UV light an acetonitrile solution of some Z-arylhydrazones (1a-e) in the presence of catalytic amounts of Ru(bpY)(2)Cl-2. We have observed the unexpected formation of the 1-aryl-5-…

RegiochemistryRuthenium catalystDrug Discovery3003 Pharmaceutical ScienceOrganic ChemistryRegioselectivityRuthenium catalystPhotochemistryDFTBiochemistryCatalysischemistry.chemical_compoundchemistryPhotochemical rearrangementDrug Discovery124-OxadiazoleAcetonitrile
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Hepatocellular carcinoma treatment over sorafenib: epigenetics, microRNAs and microenvironment. Is there a light at the end of the tunnel?

2015

Introduction: Sorafenib is currently the only approved therapy in hepatocellular carcinoma (HCC). Alternative first- and second-line treatments are a significant unmet medical need, and several biologic agents have been tested in recent years, with poor results. Therefore, angiogenic pathways and the cytokine cascade remain possible targets in HCC. Recent studies suggest a role of epigenetic processes, associated with the initiation and development of HCC. In this field, DNA methylation, micro-RNAs (miRNAs) and tumor microenvironment cells became a possible new target for HCC treatment. Areas covered: This review explains the possible role of DNA methylation and histone deacetylase inhibito…

Settore MED/06 - Oncologia MedicaClinical BiochemistrytivantinibEpigenesis GeneticAntineoplastic Agentchemistry.chemical_compoundHistone Deacetylase InhibitorDrug DiscoveryTumor MicroenvironmentMolecular Targeted TherapyplateletmicroRNALiver Neoplasmshepatocellular carcinomaSorafenibVEGFLiver NeoplasmHepatocellular carcinomaDNA methylationMolecular MedicineepigeneticHumanmedicine.drugPhenylurea CompoundSorafenibNiacinamideCarcinoma HepatocellularAntineoplastic AgentsBiologymicroRNAmedicineAnimalsHumansEpigeneticsTivantinibPharmacologyTumor microenvironmentAnimalDrug Discovery3003 Pharmaceutical SciencePhenylurea CompoundsDNA Methylationmedicine.diseasedigestive system diseasesHistone Deacetylase InhibitorsMicroRNAschemistryDrug DesignImmunologyCancer researchHistone deacetylaseExpert opinion on therapeutic targets
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Water-soluble isoindolo[2,1-a]quinoxalin-6-imines: In vitro antiproliferative activity and molecular mechanism(s) of action

2015

Abstract Water-soluble isoindoloquinoxalin (IIQ) imines and the corresponding acetates were conveniently prepared from the key intermediates 2-(2′-aminophenyl)-2H-isoindole-1-carbonitriles obtained by a Strecker reaction between substituted 1,2-dicarbaldehydes and 1,2-phenylenediamines. Both series were screened by the National Cancer Institute (Bethesda, MD) and showed potent antiproliferative activity against a panel of 60 human tumor cell lines. Several of the novel compounds showed GI50 values at a nanomolar level on the majority of the tested cell lines. Among IIQ derivatives, methoxy substituents at positions 3 and 8 or/and 9 were especially effective in impairing cell cycle progressi…

StereochemistryStrecker amino acid synthesisAntineoplastic AgentsApoptosisIsoindolo[21-a]quinoxalin-6-imineTopoisomerase I inhibitorsTopoisomerase-I InhibitorMicrotubulesTubulinCell Line TumorQuinoxalinesDrug DiscoveryHumansCytotoxic T cellCell ProliferationPharmacologyTopoisomerase I inhibitorChemistryAntitubulin agents; G-quadruplex interaction; Isoindolo[2; 1-a]quinoxalin-6-imines; Topoisomerase I inhibitors; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry; PharmacologyAntitubulin agentsDrug Discovery3003 Pharmaceutical ScienceCell CycleOrganic ChemistryWaterGeneral MedicineSettore CHIM/08 - Chimica FarmaceuticaIn vitroTelomereAntitubulin agentAntitubulin agents; G-quadruplex interaction; Isoindolo[21-a]quinoxalin-6-imines; Topoisomerase I inhibitors; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry; Pharmacology1-a]quinoxalin-6-iminesDNA Topoisomerases Type ISolubilityBiochemistryCell cultureApoptosisIsoindolo[2Cancer cellIminesG-quadruplex interactionDrug Screening Assays Antitumor
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