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A facile synthesis of deaza-analogues of the bisindole marine alkaloid topsentin.

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-carboxylates were prepared in excellent yields (82-98%) by one-pot reactions between β-dicarbonyl compounds 12a-e and 1,2-diaza-1,3-diene (DD) 13. Derivatives 10a,c-e, deazaanalogues of 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 60 human 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 lung cancer sub-panel and the SNB-75 cell line of the CNS sub-panel.
AuthorsAnna Carbone, Virginia Spanò, Barbara Parrino, Cristina Ciancimino, Orazio A Attanasi, Gianfranco Favi
JournalMolecules (Basel, Switzerland) (Molecules) Vol. 18 Issue 3 Pg. 2518-27 (Feb 26 2013) ISSN: 1420-3049 [Electronic] Switzerland
PMID23442928 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Alkaloids
  • Antineoplastic Agents
  • Imidazoles
  • Indoles
  • topsentin
Topics
  • Alkaloids (chemistry, pharmacology)
  • Antineoplastic Agents (chemistry, pharmacology)
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Humans
  • Imidazoles (chemistry, pharmacology)
  • Indoles (chemistry, pharmacology)

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