Search results for "3-d"

showing 10 items of 1132 documents

Synthesis and anti-HIV activity of 2,3-diaryl-1,3-thiazolidin-4-ones

2002

Several 1,3-thiazolidin-4-ones bearing a 2,6-dihalophenyl group at C-2 and a variously substituted phenyl ring at N-3 have been synthesized and tested as anti-HIV agents. The results of the in vitro tests showed that some of them proved to be effective inhibitors of HIV-1 replication.

Anti hiv activityAnti-HIV activityAnti-HIV Agents23-Diaryl-13-thiazolidin-4-oneChemistryStereochemistryHuman immunodeficiency virus (HIV)Pharmaceutical ScienceGeneral MedicineVirus ReplicationRing (chemistry)medicine.disease_causeChemical synthesisIn vitroCell LineThiazoleschemistry.chemical_compoundHIV-2Drug DiscoveryHIV-1NNRTIsLactammedicineHumansIl Farmaco
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Several 1,3-thiazolidin-4-ones bearing a 2,6-dihalophenyl group at C-2 and a variously substituted phenyl ring at N-3 have been synthesized and teste…

2003

Several 1,3-thiazolidin-4-ones bearing a 2,6-dihalophenyl group at C-2 and a variously substituted phenyl ring at N-3 have been synthesized and tested as anti-HIV agents. The results of the in vitro tests showed that some of them proved to be effective inhibitors of HIV-1 replication.

Anti-HIV activity23-Diaryl-13-thiazolidin-4-oneNNRTIs
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Synthesis of new 2,3-diaryl-1,3-thiazolidin-4-ones as anti-HIV agents

2004

Several 2,3-diaryl-1,3-thiazolidin-4-ones were synthesized and evaluated as anti-HIV agents. The results of the in vitro tests showed that some of them were highly effective inhibitors of HIV-1 replication at 30-50 nM concentrations with minimal cytotoxicity, thereby acting as non-nucleoside HIV-1 reverse transcriptase inhibitors (NNRTIs).

Anti-HIV activity23-diaryl-13-thiazolidin-4-oneAnti-HIV AgentsCell SurvivalT-LymphocytesDrug Evaluation PreclinicalPharmaceutical SciencePharmacologyVirus ReplicationStructure-Activity RelationshipDrug DiscoveryStructure–activity relationshipHumansCytotoxicityCell survivalAnti hiv activityMolecular StructureAnti hivChemistryvirus diseasesSettore CHIM/08 - Chimica FarmaceuticaReverse transcriptaseIn vitroThiazolesViral replicationHIV-2HIV-1NNRTIsReverse Transcriptase Inhibitors
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Eight-Membered Rings With Two Heteroatoms 1,3

2022

Eight-membered rings with two heteroatoms in a 1,3-relationship, namely 1,3-diazocine, 2H-1,3-oxazocine, 2H-1,3-thiazocine, 4H-1,3-dioxocin, 4H-1,3-oxathiocin, and 4H-1,3-dithiocin, are discussed in this chapter, that covers the literature from 2007 to October 2020 (SciFindern search) and reports the chemistry of uncondensed derivatives, heterocines fused to carbocycles and heterocycles, as well as bridged heterocines. Among eight-membered 1,3-diheterocines, 1,3-diazocines and 1,3-oxazocines are the two largest classes, based on the number of publications, mostly due to the studies of the synthesis of these cyclic systems, their pharmacological properties and/or their important industrial a…

Anti-HIV agentsCold-menthol receptor TRPM8 modulators13-DiazocineCholesterylester transfer protein (CETP) inhibitors4H-13-DithiocinSettore CHIM/08 - Chimica FarmaceuticaHistone deacetylase 6 inhibitorsEquilibrative nucleoside transporter 1 (ENT1) inhibitors4H-13-OxathiocinAnticancer agents4H-13-Dioxocin2H-13-OxazocineBiosynthetic pathways of 1 3-heterocines2H-13-Thiazocine
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CCDC 113469: Experimental Crystal Structure Determination

2000

Related Article: F.Hueso-Urena, A.L.Penas-Chamorro, M.N.Moreno-Carretero, J.M.Amigo, V.Esteve, T.Debaerdemaeker|1999|Polyhedron|18|2205|doi:10.1016/S0277-5387(99)00108-4

Aqua-((6-amino-5-formyl-13-dimethyluracil)benzoylhydrazonato)-perchlorato-copper(ii) perchlorateSpace GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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CCDC 817805: Experimental Crystal Structure Determination

2011

Related Article: M.Sarwar, A.M.Madalan, F.Lloret, M.Julve, M.Andruh|2011|Polyhedron|30|2414|doi:10.1016/j.poly.2011.06.011

Aqua-chloro-(22'-(propane-13-diylbis((nitrilo)methylylidene))-bis(6-methoxyphenolato))-iron(iii)Space GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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High chemoselectivity of CS dipolarophile in 1,3-dipolar cycloaddition of nitrilimines and 1,2,4-triazepin-5-one derivatives: experimental, theoreti…

2005

Substituted 2,7-dimethyl-3-thioxo-3,4,5,6-tetrahydro-2H-[1,2,4]triazepin-5-one reacts as a dipolarophile with several N-aryl-C-ethoxycarbonylnitrilimines, in equimolar quantities, to give, in all cases, two types of products: diethyl 3-(p-aryl)-2-[N′-(p-aryl)-N′-(2′,7′-dimethyl-5′-oxo-5′,6′-dihydro-2H-[1,2,4]triazepin-3′-yl)-hydrazino]-2,3-dihydro[1,3,4]thiadiazole-2,5-dicarboxylate (3a–3c in 20–25% yield) and ethyl 4-(p-aryl)-5-imino-1,4-dihydro[1,3,4]thiadiazole carboxylate (4a–4c in 45–50% yield). When 1:2 stoichiometry was used, the formation of product 3 (50%) was favoured. The reaction is entirely chemo- and regioselective. The structures of the compounds obtained, where aryl stands f…

ArylOrganic ChemistryRegioselectivityMedicinal chemistrychemistry.chemical_compoundchemistryNucleophileYield (chemistry)Electrophile13-Dipolar cycloadditionOrganic chemistryCarboxylatePhysical and Theoretical ChemistryChemoselectivityJournal of Physical Organic Chemistry
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Apparent absorption of solar spectral irradiance in heterogeneous ice clouds

2010

[1] Coordinated flight legs of two aircraft above and below extended ice clouds played an important role in the Tropical Composition, Cloud and Climate Coupling Experiment (Costa Rica, 2007). The Solar Spectral Flux Radiometer measured up- and downward irradiance on the high-altitude (ER-2) and the low-altitude (DC-8) aircraft, which allowed deriving apparent absorption on a point-by-point basis along the flight track. Apparent absorption is the vertical divergence of irradiance, calculated from the difference of net flux at the top and bottom of a cloud. While this is the only practical method of deriving absorption from aircraft radiation measurements, it differs from true absorption when…

Atmospheric ScienceSpectral shape analysisIrradianceSoil ScienceAquatic ScienceOceanographyice cloud absorptionAtmosphereAtmospheric radiative transfer codesGeochemistry and PetrologyEarth and Planetary Sciences (miscellaneous)3-D radiative transferAbsorption (electromagnetic radiation)Physics::Atmospheric and Oceanic PhysicsEarth-Surface ProcessesWater Science and TechnologyRemote sensingPhysicsEffective radiusRadiometerEcologyFernerkundung der AtmosphärePaleontologyForestryGeophysicsSpace and Planetary Sciencesolar spectral measurementsModerate-resolution imaging spectroradiometer
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Pimasertib Versus Dacarbazine in Patients With Unresectable NRAS-Mutated Cutaneous Melanoma: Phase II, Randomized, Controlled Trial with Crossover

2020

This study investigated the efficacy and safety of pimasertib (MEK1/MEK2 inhibitor) versus dacarbazine (DTIC) in patients with untreated NRAS-mutated melanoma. Phase II, multicenter, open-label trial. Patients with unresectable, stage IIIc/IVM1 NRAS-mutated cutaneous melanoma were randomized 2:1 to pimasertib (60 mg

Cancer ResearchGastroenterologypimasertiblaw.invention0302 clinical medicineRandomized controlled triallawClinical endpoint030212 general & internal medicineMalignant melanomaHazard ratioProgression-free survivalSciences bio-médicales et agricoleslcsh:Neoplasms. Tumors. Oncology. Including cancer and carcinogens3. Good healthDacarbazineOncology[SDV.SP.PHARMA] Life Sciences [q-bio]/Pharmaceutical sciences/Pharmacology030220 oncology & carcinogenesismedicine.symptomPimasertibmedicine.drugQuality of lifemedicine.medical_specialtyNauseaDacarbazinemalignant melanomadacarbazine[SDV.CAN]Life Sciences [q-bio]/CancerN-(2 3-dihydroxypropyl)-1-((2-fluoro-4-iodophenyl)amino)isonicotinamideNeutropeniaN-(23-dihydroxypropyl)-1-((2-fluoro-4-iodophenyl)amino)isonicotinamidelcsh:RC254-282Article03 medical and health sciences[SDV.CAN] Life Sciences [q-bio]/CancerInternal medicinemedicineProgression-free survivalAdverse effectbusiness.industry[SDV.MHEP.DERM] Life Sciences [q-bio]/Human health and pathology/Dermatologymedicine.diseaseadverse eventsCancérologiequality of lifeAdverse events[SDV.SP.PHARMA]Life Sciences [q-bio]/Pharmaceutical sciences/Pharmacologybusinessprogression-free survival[SDV.MHEP.DERM]Life Sciences [q-bio]/Human health and pathology/Dermatology
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823: 3-deazaneplanocin A (DZNep), an inhibitor of histone methyltransferase EZH2, induces apoptosis and reduces cell migration in chondrosarcoma cells

2014

Cancer Researchchemistry.chemical_compoundOncologyChemistryApoptosisHistone methyltransferaseEZH2medicineCancer research3-Deazaneplanocin ACell migrationChondrosarcomamedicine.diseaseEuropean Journal of Cancer
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