Synthesis of flavone-2'-carboxylic acid analogues as potential antitumor agents.
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.
Valenti
P
P
Department of Pharmaceutical Sciences, University of Bologna, Italy.
Bisi
A
A
Rampa
A
A
Gobbi
S
S
Belluti
F
F
Da Re
P
P
Cima
L
L
Carrara
M
M
D000276:Adjuvants, Immunologic / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002264:Carboxylic Acids / Q000737:chemistry*; D004354:Drug Screening Assays, Antitumor; D005419:Flavonoids / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D017737:Macrophages, Peritoneal / Q000187:drug effects; D051379:Mice; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000276:Adjuvants, Immunologic; D000970:Antineoplastic Agents; D002264:Carboxylic Acids; D005419:Flavonoids; C049328:flavone acetic acid