Search results for "Anilide"

showing 10 items of 40 documents

Kinase Inhibitors in Multitargeted Cancer Therapy

2017

The old-fashioned anticancer approaches, aiming in arresting cancer cell proliferation interfering with non-specific targets (e.g. DNA), have been replaced, in the last decades, by more specific target oriented ones. Nonetheless, single-target approaches have not always led to optimal outcomes because, for its complexity, cancer needs to be tackled at various levels by modulation of several targets. Although at present, combinations of individual single-target drugs represent the most clinically practiced therapeutic approaches, the modulation of multiple proteins by a single drug, in accordance with the polypharmacological strategy, has become more and more appealing. In the perspective of…

0301 basic medicineDrugNiacinamideIndolesPyridinesmedia_common.quotation_subjectPharmacologyBioinformaticsBiochemistryReceptor tyrosine kinase03 medical and health sciencesCrizotinibPiperidinesMultitargeted drugs anticancer agents polypharmacology tyrosine kinase receptors oncogene addiction tumor microenvironment FDA-approved drugsNeoplasmsDrug DiscoverymedicineSunitinibHumansAnilidesPyrrolesProtein Kinase Inhibitorsmedia_commonPharmacologyTumor microenvironmentbiologybusiness.industryPhenylurea CompoundsOrganic ChemistryImidazolesCancerReceptor Protein-Tyrosine KinasesSorafenibmedicine.diseaseOncogene AddictionSettore CHIM/08 - Chimica FarmaceuticaClinical trialPyridazines030104 developmental biologyMechanism of actionbiology.proteinImatinib MesylateQuinazolinesMolecular MedicinePyrazolesmedicine.symptombusinessTyrosine kinase
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Cabozantinib targets bone microenvironment modulating human osteoclast and osteoblast functions

2016

Cabozantinib, a c-MET and vascular endothelial growth factor receptor 2 inhibitor, demonstrated to prolong progression free survival and improve skeletal disease-related endpoints in castration-resistant prostate cancer and in metastatic renal carcinoma. Our purpose is to investigate the direct effect of cabozantinib on bone microenvironment using a total human model of primary osteoclasts and osteoblasts.Osteoclasts were differentiated from monocytes isolated from healthy donors; osteoblasts were derived from human mesenchymal stem cells obtained from bone fragments of orthopedic surgery patients. Osteoclast activity was evaluated by tartrate resistant acid phosphatase (TRAP) staining and …

0301 basic medicinePyridines -- pharmacologyPyridinesPyridineImmunoenzyme TechniqueOsteoclastsApoptosisRANK Ligand -- genetics -- metabolismImmunoenzyme Techniqueschemistry.chemical_compoundBone Resorption -- drug therapy -- metabolism -- pathology0302 clinical medicineOsteogenesisCathepsin KMedicineAnilidesAnilides -- pharmacologyOsteoprotegerin -- genetics -- metabolismOsteoclasts -- cytology -- drug effects -- physiologyHuman primary cellCells CulturedTartrate-resistant acid phosphataseReceptor Activator of Nuclear Factor-kappa B -- genetics -- metabolismbiologyProto-Oncogene Proteins c-met -- genetics -- metabolismReceptor Activator of Nuclear Factor-kappa BReverse Transcriptase Polymerase Chain ReactionOsteoblastOsteogenesiOsteoblastCell DifferentiationSciences bio-médicales et agricolesProto-Oncogene Proteins c-metOsteoblasts -- cytology -- drug effects -- physiologymedicine.anatomical_structureCell Differentiation -- drug effectsOncologyRANKL030220 oncology & carcinogenesishuman primary cellsOsteoclastosteoprotegerin (OPG)bone microenvironmentHumanResearch Papermusculoskeletal diseasesmedicine.medical_specialtyCabozantinibBlotting WesternOsteogenesis -- drug effects -- physiologyReal-Time Polymerase Chain ReactionBone resorption03 medical and health sciencesOsteoprotegerinOsteoclastcabozantinibInternal medicineHumansRNA MessengerBone ResorptionCell ProliferationOsteoblastsbusiness.industryRANK LigandAnilideOsteoprotegerinApoptosiBone microenvironment; Cabozantinib; Human primary cells; Osteoprotegerin (OPG); Receptor activator of nuclear factor-kb ligand (RANKL); Anilides; Apoptosis; Blotting Western; Bone Resorption; Cell Differentiation; Cell Proliferation; Cells Cultured; Humans; Immunoenzyme Techniques; Osteoblasts; Osteoclasts; Osteogenesis; Osteoprotegerin; Proto-Oncogene Proteins c-met; Pyridines; RANK Ligand; RNA Messenger; Real-Time Polymerase Chain Reaction; Receptor Activator of Nuclear Factor-kappa B; Reverse Transcriptase Polymerase Chain Reaction; Oncology030104 developmental biologyEndocrinologychemistrybiology.proteinbusinessRNA Messenger -- geneticsreceptor activator of nuclear factor-kb ligand (RANKL)
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Aqueous coefficient calculations for chemicals and drugs

1999

Aqueous functional group activity coefficients (AQUAFAC) is a group‐contribution method for estimating the aqueous coefficients. We have written a program for the calculation of these coefficients. The solubility S w of alkanes shows variation of 8 orders of magnitude. The comparison with experiment shows that AQUAFAC gives good S w estimations. For 4'‐substituted acetanilides, I‐, Br‐, nitro‐, Cl‐, F‐ and methoxy‐substituents decrease S w, while formyl‐ and amino‐substituents increase S w. For acetaminophen esters, S w decreases from the acetate to the decanoate. The S w of 29 barbiturates shows typical errors of 0.4 log S w units. For the cyclo‐alkane‐l’,5‐spirobarbituric acids, S w decre…

Activity coefficientAqueous solutionHealth Toxicology and MutagenesisAnalytical chemistryPollutionCyclopropanechemistry.chemical_compoundchemistryNitroEnvironmental ChemistryCyclooctaneOrganic chemistryOrders of magnitude (speed)SolubilityAcetanilideToxicological & Environmental Chemistry
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Lorcainide. I. Saturable presystemic elimination.

1979

AdultMaleBenzeneacetamidesAdministration OralPharmacologyHepatic VeinsIn Vitro TechniquesPulmonary ArteryLorcainidePiperidinesMedicineHumansPharmacology (medical)Aorta AbdominalAortaAgedPharmacologybusiness.industryArrhythmias CardiacBlood ProteinsMiddle AgedBloodInjections IntravenousAcetanilidesFemalebusinessAnti-Arrhythmia Agentsmedicine.drugProtein BindingClinical pharmacology and therapeutics
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Lorcainide; II. Plasma concentration-effect relationship

1979

AdultMalePharmacologyChromatographybusiness.industryBenzeneacetamidesAdministration OralArrhythmias CardiacIn Vitro TechniquesMiddle AgedLorcainideElectrocardiographyPiperidinesInjections IntravenousPlasma concentrationmedicineHumansAcetanilidesFemaleInfusions ParenteralPharmacology (medical)businessAnti-Arrhythmia AgentsAgedmedicine.drugClinical Pharmacology & Therapeutics
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Cemiplimab in locally advanced basal cell carcinoma after hedgehog inhibitor therapy: an open-label, multi-centre, single-arm, phase 2 trial.

2021

Summary Background Before February, 2021, there was no standard treatment regimen for locally advanced basal cell carcinoma after first-line hedgehog inhibitor (HHI) therapy. Cemiplimab, a PD-1 antibody, is approved for treatment of advanced cutaneous squamous cell carcinoma and has shown clinical activity as monotherapy in first-line non-small-cell lung cancer. Here, we present the primary analysis data of cemiplimab in patients with locally advanced basal cell carcinoma after HHI therapy. Methods We did an open-label, multicentre, single-arm, phase 2 trial across 38 outpatient clinics, primarily at academic medical centres, in Canada, Europe, and the USA. Eligible patients (aged ≥18 years…

AdultMalemedicine.medical_specialtySkin NeoplasmsPyridinesProgrammed Cell Death 1 ReceptorVismodegibAntibodies Monoclonal Humanized030207 dermatology & venereal diseases03 medical and health sciences0302 clinical medicineInternal medicineAntineoplastic Combined Chemotherapy ProtocolsmedicineCarcinomaClinical endpointOutpatient clinicHumansBasal cell carcinomaAnilidesHedgehog ProteinsLung cancerImmune Checkpoint InhibitorsAgedbusiness.industryStandard treatmentMiddle Agedmedicine.diseaseRegimenOncologyCarcinoma Basal CellDrug Resistance Neoplasm030220 oncology & carcinogenesisFemaleNeoplasm Recurrence LocalSettore MED/35 - MALATTIE CUTANEE E VENEREEbusinessmedicine.drugThe Lancet. Oncology
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Involvement of cholinergic nicotinic receptors in the menthol-induced gastric relaxation.

2014

We have previously demonstrated that menthol reduces murine gastric tone in part through a neural mechanism, involving adrenergic pathways and reduction of ongoing release of acetylcholine from enteric nerves. In the present study we aimed to verify whether the gastric relaxation to menthol may be triggered by interaction with neural receptors or ionic channels proteins, such as transient receptor potential (TRP)-melastatin8 (TRPM8), TRP-ankyrin 1 (TRPA1), 5-hydroxytriptamine 3 (5-HT3) receptor or cholinergic nicotinic receptors. Spontaneous mechanical activity was detected in vitro as changes in intraluminal pressure from isolated mouse stomach. Menthol (0.3-30 mM) induced gastric relaxati…

AgonistMalemedicine.medical_specialtySerotoninmedicine.drug_classDimethylphenylpiperaziniumMuscle RelaxationTRPM Cation ChannelsPharmacologyReceptors NicotinicSettore BIO/09 - Fisiologiachemistry.chemical_compoundMiceGanglion type nicotinic receptorTransient Receptor Potential ChannelsIsothiocyanatesInternal medicinemedicineTRPM8AnimalsSerotonin 5-HT3 Receptor AntagonistsRNA MessengerTRPA1 Cation ChannelPharmacologyStomachmenthol gastric relaxation TRPM8 TRPA1 nicotinic receptorsReceptor antagonistOndansetronMice Inbred C57BLMentholEndocrinologyNicotinic agonistchemistryPurinesHexamethoniumAcetanilidesAlpha-4 beta-2 nicotinic receptorGastrointestinal Motilitymedicine.drugEuropean journal of pharmacology
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Anomalous temperature dependence of the IR spectrum of polyalanine

1997

Abstract We have studied the temperature dependence of the infrared spectra of acetanilide (ACN), tryptophan–(alanine) 15 , and tyrosine–(alanine) 15 . No sidebands of the amide-I vibration were observed in the polypeptides, but two anomalous sidebands of the NH stretch with a similar temperature dependence as that of the anomalous amide-I vibrational mode at 1650 cm −1 of crystalline ACN were detected. Fermi resonance combined with the appearance of a red-shifted sideband of NH stretch through coupling to lattice modes seems to explain this band structure. Observations are indicative of excitons that may occur in polypeptides as well as in single crystals of ACN.

AlaninePhysics::Biological PhysicsQuantitative Biology::BiomoleculesSidebandChemistryExcitonGeneral Physics and AstronomyInfrared spectroscopy02 engineering and technology021001 nanoscience & nanotechnology01 natural sciencesMolecular physics3. Good healthchemistry.chemical_compoundNuclear magnetic resonanceLattice (order)0103 physical sciencesFermi resonancePhysical and Theoretical Chemistry010306 general physics0210 nano-technologyElectronic band structureAcetanilideChemical Physics Letters
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Apoptosis induced in HepG2 cells by the synthetic cannabinoid WIN: involvement of the transcription factor PPARgamma.

2008

It has recently been shown that cannabinoids induce growth inhibition and apoptosis in different tumour cell lines. In the current study, the effects of WIN 55,212-2 (WIN), a synthetic and potent cannabinoid receptor agonist, are investigated in hepatoma HepG2 cells and a possible signal transduction pathway is proposed. In these cells, WIN induces a clear apoptotic effect which was accompanied by up-regulation of the death-signalling factors Bax, Bcl-X(S), t-Bid and down-regulation of the survival factors survivin, phospho-AKT, Hsp72 and Bcl-2. Moreover, WIN-induced apoptosis is associated with JNK/p38 MAPK pathway activation and mitochondrial depolarisation demonstrated by a cytofluorimet…

Cannabinoid receptorCarcinoma HepatocellularCell SurvivalPyridinesmedicine.medical_treatmentp38 mitogen-activated protein kinasesMorpholinesApoptosisBiologyNaphthalenesBiochemistryReceptor Cannabinoid CB2Membrane Microdomainscannabinoids PPARgamma factor apoptosis cancer cellsSettore BIO/10 - BiochimicaCell Line TumorSurvivinmedicineHumansAnilidesViability assayCannabinoidsLiver NeoplasmsGeneral MedicineCell biologyBenzoxazinesPPAR gammaApoptosisCancer cellBenzamidesCannabinoidSignal transductionApoptosis Regulatory ProteinsProtein KinasesSignal TransductionBiochimie
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Genetic instability in calamondin (Citrus madurensis Lour.) plants derived from somatic embryogenesis induced by diphenylurea derivative

2007

Somatic embryos were regenerated in vitro from calamondin style-stigma explants cultured in the presence of N (6)-benzylaminopurine (BAP) cytokinin and three synthetic phenylurea derivatives, N-(2-chloro-4-pyridyl)-N-phenylurea (4-CPPU), N-phenyl-N'-benzothiazol-6-ylurea (PBU) and N,N'-bis-(2,3-methilendioxyphenyl)urea (2,3-MDPU). The phenylurea derivative compounds tested at micromolar level (12 muM) were able to induce a percentage of responsive explants significantly higher from that obtained with BAP and hormone-free (HF) conditions. In order to verify the genetic stability of the regenerants, 27 plants coming from different embryogenic events were randomly selected from each different …

CitrusSomatic embryogenesisMutantPlant ScienceBiologyGenetic polymorphismsSomaclonal variationTissue Culture Techniqueschemistry.chemical_compoundGene Expression Regulation PlantBotanygenetic polymorphismmolecular markerPolymorphism GeneticMolecular markersGeneral MedicineSomaclonal variabilitybiology.organism_classificationMolecular biologyIn vitroCulture MediaRutaceaechemistryMutagenesisCytokininmutationAgronomy and Crop ScienceCarbanilidesDNAMutationsExplant culturePlant regeneration
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