Synthesis and antiproliferative activity of [1,2,3,5]tetrazino[5,4-a]indoles, a new class of azolo-tetrazinones.
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.
Barraja
Paola
P
Dipartimento Farmacochimico Tossicologico e Biologico, Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy.
Diana
Patrizia
P
Lauria
Antonino
A
Montalbano
Alessandra
A
Almerico
Anna Maria
AM
Dattolo
Gaetano
G
Cirrincione
Girolamo
G
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
D000970:Antineoplastic Agents; D007211:Indoles