A Facile Synthesis of Deaza-Analogues of the Bisindole Marine Alkaloid Topsentin

Virginia Spano', Cristina Ciancimino, Barbara Parrino, Anna Carbone, Gianfranco Favi, Orazio A. Attanasi

Risultato della ricerca: Articlepeer review

14 Citazioni (Scopus)

Abstract

A series of substituted ethyl 1-[(tert-butoxycarbonyl)amino]-2-methyl-5-(1-methyl-1H-indol-3-yl)-4-[(1-methyl-1H-indol-3-yl)carbonyl]-1H-pyrrole-3-carboxylateswere prepared in excellent yields (82-98%) by one-pot reactions between β-dicarbonylcompounds 12a–e and 1,2-diaza-1,3-diene (DD) 13. Derivatives 10a,c–e, deazaanaloguesof the bis-indole alkaloid topsentin, screened by the National Cancer Institute (Bethesda,MD, USA) in the in vitro one dose primary anticancer assay against a panel of about 60human tumor cell lines, showed no significant activity, with the exception of compound 9e,which showed moderate activity against the HOP-92 cell line of the non small cell lungcancer sub-panel and the SNB-75 cell line of the CNS sub-panel.
Lingua originaleEnglish
pagine (da-a)2518-2527
Numero di pagine10
RivistaMolecules
Volume18
Stato di pubblicazionePublished - 2013

All Science Journal Classification (ASJC) codes

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  • ???subjectarea.asjc.1600.1602???
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  • ???subjectarea.asjc.3000.3003???
  • ???subjectarea.asjc.3000.3002???
  • ???subjectarea.asjc.1600.1606???
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