Differential antiproliferative activity of new benzimidazole-4,7-diones.
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.
Garuti
Laura
L
Department of Pharmaceutical Science, University of Bologna, via Belmeloro 6, Bologna 40126, Italy. lauga@alma.unibo.it
Roberti
Marinella
M
Pizzirani
Daniela
D
Pession
Annalisa
A
Leoncini
Emanuela
E
Cenci
Valentina
V
Hrelia
Silvana
S
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020014:K562 Cells; D007659:Ketones / Q000138:chemical synthesis* / Q000494:pharmacology*; D015394:Molecular Structure; D019384:Nucleic Acid Synthesis Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D001562:Benzimidazoles; D007659:Ketones; D019384:Nucleic Acid Synthesis Inhibitors