Synthesis and biological activity of some rigid analogues of flavone-8-acetic acid.
Some rigid analogues of flavone-8-acetic acid are described. Direct in vitro toxicity of the synthesised compounds was evaluated towards four tumoral cell lines and the ability of these compounds to stimulate mouse peritoneal macrophages in culture to become tumoricidal (indirect toxicity) was also studied. All compounds were able to induce direct cytotoxicity only at very high concentrations but showed a remarkable indirect activity. In particular compound 4d was able to significantly increase macrophage lytic properties and has been selected for further investigations.
Valenti
P
P
Department of Pharmaceutical Sciences, University Bologna, Italy. pvalenti@alma.unibo.it
Bisi
A
A
Rampa
A
A
Belluti
F
F
Gobbi
S
S
Zampiron
A
A
Carrara
M
M
D000818:Animals; D002455:Cell Division / Q000187:drug effects; D002478:Cells, Cultured; D005419:Flavonoids / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D006801:Humans; D017737:Macrophages, Peritoneal / Q000187:drug effects / Q000276:immunology; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D014407:Tumor Cells, Cultured
D005419:Flavonoids; C049328:flavone acetic acid