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Synthesis and antiproliferative activity of the ring system [1,2]oxazolo[4,5-g]indole.

2012

Brand new ring: A series of 27 derivatives of the new ring system [1,2]oxazolo[4,5-g]indole were conveniently prepared and tested at the NCI for antiproliferative studies. Several of them showed good inhibitory activity toward all tested cell lines, reaching GI50 values generally at the micromolar and sub-micromolar levels and in some cases at nanomolar concentrations. The mean GI50 values, calculated on the full panel, were in the range 0.25-7.08 μM.

antiproliferative activityIndolesStereochemistryhydroxylamine hydrochloridesAntineoplastic AgentsRing (chemistry)Biochemistrychemistry.chemical_compoundStructure-Activity RelationshipCell Line TumorNeoplasms2]oxazolo[4Drug Discoveryantiproliferative activity; combretastatin A-4; enaminoketones; hydroxylamine hydrochlorides; [1; 2]oxazolo[4; 5-g]indolesStructure–activity relationshipHumanscombretastatin A-4General Pharmacology Toxicology and PharmaceuticsOxazolesCell ProliferationPharmacologyCombretastatin A-4Indole testantiproliferative activity combretastatin A-4 enaminoketones hydroxylamine hydrochlorides[12]oxazolo[45-g]indolesOrganic ChemistrySettore CHIM/08 - Chimica Farmaceuticachemistry5-g]indolesenaminoketonesMolecular Medicine[1Drug Screening Assays AntitumorChemMedChem
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