Antitumor activity of diethynylfluorene derivatives of gold(I)

End-capping the diethynylfluorene unit with gold(I) moieties could significantly strengthen its cytotoxic activity on human cancer cells. Further study of the gold(I) derivative demonstrated its in vivo antitumor activity using Hep3B human hepatocellular carcinoma model with limited adverse effects on vital organs including liver and kidney. A list of diethynylfluorenes and their gold(I) derivatives have been studied for their antitumor activity as a function of their structure–activity relationships. End-capping the fluoren-9-one unit with gold(I) moieties could significantly strengthen the cytotoxic activity in vitro on three human cancer cell lines with induction of reactive oxygen species generation on Hep3B hepatocellular carcinoma cells and exhibit attractive antitumor activity from in vivo nude mice Hep3B xenograft model with limited adverse effects on vital organs including liver and kidney.