title: Synthesis and antiproliferative activity of [1,2,3,5]tetrazino[5,4-a]indoles, a new class of azolo-tetrazinones.
abstract: 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.
authors.affiliation: Dipartimento Farmacochimico Tossicologico e Biologico, Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy.
authors.forename: Paola
authors.initials: P
authors.lastname: Barraja
authors.forename: Patrizia
authors.initials: P
authors.lastname: Diana
authors.forename: Antonino
authors.initials: A
authors.lastname: Lauria
authors.forename: Alessandra
authors.initials: A
authors.lastname: Montalbano
authors.forename: Anna Maria
authors.initials: AM
authors.lastname: Almerico
authors.forename: Gaetano
authors.initials: G
authors.lastname: Dattolo
authors.forename: Girolamo
authors.initials: G
authors.lastname: Cirrincione
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms; D002289:Carcinoma, Non-Small-Cell Lung; D045744:Cell Line, Tumor; D016543:Central Nervous System Neoplasms; D003110:Colonic Neoplasms; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007938:Leukemia; D008297:Male; D008545:Melanoma; D015394:Molecular Structure; D010051:Ovarian Neoplasms
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles