Flavonoid compounds: a review of anticancer properties and interactions with cis ‐diamminedichloroplatinum(II)

Flavonoid compounds, especially quercetin and genistein, have antitumor activity. These compounds are cytotoxic to cancer cells but have no or insignificant activity in normal cells. These beneficial properties prompted synthesis of flavonoid synthetic derivatives, e.g., flavopiridol; 5‐amino‐2,3‐fluorophenyl)‐6,8‐difluoro‐7‐methyl‐4H‐1‐benzopyran‐4‐one; B43‐genistein and EGF‐genistein). cis ‐DDP ( cis ‐diamminedichloroplatinum(II)) is one of the most effective drugs used for chemotherapy, but its actions are limited by many side effects. Beneficial synergistic effects of flavonoids (e.g., quercetin, genistein, butein, tannic acid) and cis ‐DDP were found in cis ‐DDP‐sensitive and resistant cancer cells that resulted in a lower toxicity for cis ‐DDP. Further studies focused on the synthesis of complexes of compounds belonging to different groups, e.g., cis ‐bis(3‐aminoflavone)dichloroplatinum(II) where introduction of the flavone ligand altered the DNA‐binding properties of the complex as compared to cis ‐DDP alone. The beneficial anticancer and antioxidant properties of flavonoids and their synthetic derivatives have prompted further research on the synergistic interactions of these compounds with routinely applied chemotherapeutic drugs, e.g. cis ‐DDP. Drug Dev. Res. 63:200–211, 2004. © 2004 Wiley‐Liss, Inc.