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.

BARRAJA, P., DIANA, P., LAURIA, A., MONTALBANO, A., ALMERICO, A.M., DATTOLO, G., et al. (2005). Synthesis and Antiproliferative Activity of [1,2,3,5]tetrazino[5,4-a]indoles, a New Class of Azolo-tetrazinones. BIOORGANIC & MEDICINAL CHEMISTRY, 13(2), 295-300 [10.1016/j.bmc.2004.10.028].

Synthesis and Antiproliferative Activity of [1,2,3,5]tetrazino[5,4-a]indoles, a New Class of Azolo-tetrazinones

BARRAJA, Paola;DIANA, Patrizia;LAURIA, Antonino;MONTALBANO, Alessandra;ALMERICO, Anna Maria;DATTOLO, Gaetano;CIRRINCIONE, Girolamo
2005-01-01

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. 2004 Elsevier Ltd. All rights reserved.
2005
BARRAJA, P., DIANA, P., LAURIA, A., MONTALBANO, A., ALMERICO, A.M., DATTOLO, G., et al. (2005). Synthesis and Antiproliferative Activity of [1,2,3,5]tetrazino[5,4-a]indoles, a New Class of Azolo-tetrazinones. BIOORGANIC & MEDICINAL CHEMISTRY, 13(2), 295-300 [10.1016/j.bmc.2004.10.028].
File in questo prodotto:
File Dimensione Formato  
antiproliferative.pdf

Solo gestori archvio

Descrizione: Articolo
Dimensione 283.8 kB
Formato Adobe PDF
283.8 kB Adobe PDF   Visualizza/Apri   Richiedi una copia

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10447/20666
Citazioni
  • ???jsp.display-item.citation.pmc??? 1
  • Scopus 25
  • ???jsp.display-item.citation.isi??? 21
social impact