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. (C) 2000 Elsevier Science Ltd.
Valenti P., Bisi A., Rampa A., Belluti F., Gobbi S., Zampiron A., et al. (2000). Synthesis and biological activity of some rigid analogues of flavone-8- acetic acid. BIOORGANIC & MEDICINAL CHEMISTRY, 8(1), 239-246 [10.1016/S0968-0896(99)00282-5].
Synthesis and biological activity of some rigid analogues of flavone-8- acetic acid
Valenti P.
;Bisi A.;Rampa A.;Belluti F.;Gobbi S.;
2000
Abstract
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. (C) 2000 Elsevier Science Ltd.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
