6533b82bfe1ef96bd128d6ac

RESEARCH PRODUCT

Synthesis of [1,2]oxazolo[5,4-e]indazoles as antitumour agents

Daniele GiallombardoPatrizia DianaAnna CarbonePaola BarrajaAlessandra MontalbanoVirginia SpanòBarbara ParrinoGirolamo Cirrincione

subject

Annulation2]Oxazolo[5StereochemistryOrganic ChemistryHydroxylamine hydrochlorideAntiproliferative activityRing (chemistry)Hydroxylamine HydrochlorideBiochemistryMedicinal chemistrySettore CHIM/08 - Chimica Farmaceutica[12]Oxazolo[54-e]indazoles Enaminoketones Hydroxylamine hydrochloride Antiproliferative activitychemistry.chemical_compoundEnaminoketoneschemistryDrug Discovery4-e]indazoles[1; 2]Oxazolo[5; 4-e]indazoles; Enaminoketones; Hydroxylamine hydrochloride; Antiproliferative activity[1Oxazole

description

Abstract A series of 40 derivatives of the [1,2]oxazolo[5,4-e]indazoles ring system have been prepared with good yields using a versatile and convenient route. Annelation of the [1,2]oxazole ring on the indazole-4-one system was achieved by reaction of the corresponding enaminoketones with hydroxylamine hydrochloride. Derivatives of the title ring system were tested by the National Cancer Institute of Bethesda and one of them (13t) showed growth-inhibitor activity against all the 54 human tumour cell lines generally at low micromolar concentrations.

yearjournalcountryeditionlanguage
2013-08-01
10.1016/j.tet.2013.05.083http://hdl.handle.net/10447/80223