6533b859fe1ef96bd12b7803

RESEARCH PRODUCT

Synthesis and antiproliferative activity of [1,2,3,5]tetrazino[5,4-a]indoles, a new class of azolo-tetrazinones.

Girolamo CirrincionePatrizia DianaGaetano DattoloPaola BarrajaAnna Maria AlmericoAlessandra MontalbanoAntonino Lauria

subject

MaleIndolesStereochemistryClinical BiochemistryPharmaceutical ScienceAntineoplastic AgentsBreast NeoplasmsBiochemistryChemical synthesisCentral Nervous System Neoplasmschemistry.chemical_compoundCarcinoma Non-Small-Cell LungCell Line TumorDrug DiscoverymedicineHumansMolecular BiologyMelanomaOvarian NeoplasmsLeukemiaMolecular StructureArylMelanomaOrganic ChemistryCancerDiazoindoles Azolotetrazinones Antiproliferative activity Tetrazino-indolesmedicine.diseaseIn vitroSensitive cellchemistryCell cultureColonic NeoplasmsMolecular MedicineFemaleDrug Screening Assays AntitumorOvarian cancer

description

Eight derivatives of the new ring system [1,2,3,5]tetrazino[5,4-a]indole-4-one 7, were synthesised in good yields by reaction of 2-diazoindoles with alkyl or aryl isocyanates. Compounds 7 were screened at National Cancer Institute (NCI) for their activity against a panel of approximately 60 human tumour cell lines. Some of them showed antiproliferative activity having generally GI50 in the micromolar range. The most sensitive cell lines were SF-295, SNB-75 and SF-539 of the CNS cancer sub-panel, SR of the leukaemia sub-panel, UACC-62 of the melanoma sub-panel and OVCAR-4 of the ovarian cancer sub-panel. 2004 Elsevier Ltd. All rights reserved.

yearjournalcountryeditionlanguage
2004-08-03Bioorganicmedicinal chemistry
10.1016/j.bmc.2004.10.028https://pubmed.ncbi.nlm.nih.gov/15598552