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

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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 reactionof 2-diazoindoles with alkyl or aryl isocyanates. Compounds 7 were screened at National Cancer Institute (NCI) for their activityagainst a panel of approximately 60 human tumour cell lines. Some of them showed antiproliferative activity having generallyGI50 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 theleukaemia sub-panel, UACC-62 of the melanoma sub-panel and OVCAR-4 of the ovarian cancer sub-panel. 2004 Elsevier Ltd. All rights reserved.
Lingua originaleEnglish
pagine (da-a)295-300
Numero di pagine6
RivistaBIOORGANIC & MEDICINAL CHEMISTRY
Volume13
Stato di pubblicazionePublished - 2005

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All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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