Synthesis and anticancer activity of new pyrrolocarbazoles and pyrrolo-beta-carbolines.

Abstract

'Bended' 1, 3 or 'linear' 2 pyrrolidino-fused (aza)carbazoles were prepared and screened towards a few cancer-related targets. Whereas 'bended' derivatives 1 and 3 proved to be weakly toxic, several members of the 'linear' family strongly interact with DNA, especially derivative 28a.

• Authors: M Laronze, M Boisbrun, S Léonce, B Pfeiffer, P Renard, O Lozach, L Meijer, A Lansiaux, C Bailly, J Sapi, J-Y Laronze
• Journal: Bioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 13 Issue 6 Pg. 2263-83 (Mar 15 2005) ISSN: 0968-0896 [Print] England
• PMID: 15830466 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Carbazoles
• Carbolines
• Enzyme Inhibitors
• Indoles
• Pyrroles
• Topoisomerase I Inhibitors
• indole
• DNA
• Glycogen Synthase Kinase 3 beta
• CDC2 Protein Kinase
• Glycogen Synthase Kinase 3
• glycogen synthase kinase 3 alpha
• DNA Topoisomerases, Type I

Topics

• Animals
• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology, toxicity)
• CDC2 Protein Kinase (antagonists & inhibitors, metabolism)
• Carbazoles (chemical synthesis, chemistry, pharmacology, toxicity)
• Carbolines (chemical synthesis, chemistry, pharmacology, toxicity)
• Cell Cycle (drug effects)
• Cell Line, Tumor
• DNA (genetics, metabolism)
• DNA Footprinting
• DNA Topoisomerases, Type I (metabolism)
• Enzyme Inhibitors (chemical synthesis, chemistry, pharmacology, toxicity)
• Glycogen Synthase Kinase 3 (antagonists & inhibitors, metabolism)
• Glycogen Synthase Kinase 3 beta
• Indoles (chemistry)
• Inhibitory Concentration 50
• Mice
• Molecular Structure
• Nucleic Acid Denaturation
• Pyrroles (chemistry)
• Structure-Activity Relationship
• Temperature
• Titrimetry
• Topoisomerase I Inhibitors