Some flavone-2'-carboxylic acid analogues are described. Direct in vitro toxicity of the synthesized 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. Direct cytotoxic activity was very low for all derivatives. However, almost all compounds showed a remarkable increase of indirect cytotoxicity. In particular, compound 3i, which has an F atom in the 7 position of the flavone ring, was able to increase significantly the macrophage's lytic properties, and has been selected for further investigations.
Synthesis of flavone-2'-carboxylic acid analogues as potential antitumor agents / Valenti P.; Bisi A.; Rampa A.; Gobbi S.; Belluti F.; Re P.D.; Cima L.; Carrara M.. - In: ANTI-CANCER DRUG DESIGN. - ISSN 0266-9536. - STAMPA. - 13:8(1998), pp. 881-892.
Synthesis of flavone-2'-carboxylic acid analogues as potential antitumor agents
Valenti P.;Bisi A.;Rampa A.;Gobbi S.;Belluti F.;
1998
Abstract
Some flavone-2'-carboxylic acid analogues are described. Direct in vitro toxicity of the synthesized 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. Direct cytotoxic activity was very low for all derivatives. However, almost all compounds showed a remarkable increase of indirect cytotoxicity. In particular, compound 3i, which has an F atom in the 7 position of the flavone ring, was able to increase significantly the macrophage's lytic properties, and has been selected for further investigations.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
