Synthesis and Antiproliferative Activity of [1,2,3,5]tetrazino[5,4-a]indoles, a New Class of Azolo-tetrazinones
- Autori: Barraja, P.; Diana, P.; Lauria, A.; Montalbano, A.; Almerico, A.; Dattolo, G.; Cirrincione, G.
- Anno di pubblicazione: 2005
- Tipologia: Articolo in rivista (Articolo in rivista)
- OA Link: http://hdl.handle.net/10447/20666
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.