6533b7ddfe1ef96bd1273603

RESEARCH PRODUCT

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

Girolamo CirrincioneAnna CarbonePatrizia DianaVirginia SpanòBarbara ParrinoLibero CaracausiAlessandra MontalbanoPaola Barraja

subject

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 Antitumor

description

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.

yearjournalcountryeditionlanguage
2012-01-01ChemMedChem
10.1002/cmdc.201200296https://pubmed.ncbi.nlm.nih.gov/22915307