Differential antiproliferative activity of new benzimidazole-4,7-diones

Laura Garuti; Marinella Roberti; Daniela Pizzirani; Annalisa Pession; Emanuela Leoncini; Valentina Cenci; Silvana Hrelia

doi:10.1016/j.farmac.2004.04.001

Differential antiproliferative activity of new benzimidazole-4,7-diones

Farmaco. 2004 Aug;59(8):663-8. doi: 10.1016/j.farmac.2004.04.001.

Authors

Laura Garuti¹, Marinella Roberti, Daniela Pizzirani, Annalisa Pession, Emanuela Leoncini, Valentina Cenci, Silvana Hrelia

Affiliation

¹ Department of Pharmaceutical Science, University of Bologna, via Belmeloro 6, Bologna 40126, Italy. [email protected]

PMID: 15262537
DOI: 10.1016/j.farmac.2004.04.001

Abstract

Ten benzimidazole-4,7-diones were synthesized and tested in vitro on two tumor cell lines. Several compounds showed a significant antiproliferative activity on K562 cells, although to a different extent, whereas compound 1i showed a highly significant activity on SW620 cells, comparable to that of doxorubicin. Both the substituents in the quinone ring and the position of the nitrogen atom in the pyridine moiety play a crucial role for the biological activity.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / pharmacology*
Benzimidazoles / chemical synthesis*
Benzimidazoles / pharmacology*
Cell Division / drug effects
Cell Line, Tumor
Cell Survival / drug effects
Drug Screening Assays, Antitumor
Humans
K562 Cells
Ketones / chemical synthesis*
Ketones / pharmacology*
Molecular Structure
Nucleic Acid Synthesis Inhibitors / chemical synthesis
Nucleic Acid Synthesis Inhibitors / pharmacology
Structure-Activity Relationship

Substances

Antineoplastic Agents
Benzimidazoles
Ketones
Nucleic Acid Synthesis Inhibitors