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Antitumor activity of diethynylfluorene derivatives of gold(I) |
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| Authors: | Chung-Hin Chui Raymond Siu-Ming Wong Roberto Gambari Gregory Yin-Ming Cheng Marcus Chun-Wah Yuen Kit-Wah Chan See-Wai Tong Fung-Yi Lau Paul Bo-San Lai Kim-Hung Lam Cheuk-Lam Ho Chi-Wai Kan Kelvin Sze-Yin Leung Wai-Yeung Wong |
| Affiliation: | 1. Institute of Textiles and Clothing, Hong Kong Polytechnic University, Hung Hom, Hong Kong, People’s Republic of China;2. Department of Medicine and Therapeutics, Li Ka Shing Medical Sciences Building, Prince of Wales Hospital, The Chinese University of Hong Kong, Hong Kong, People’s Republic of China;3. BioPharmaNet, Department of Biochemistry and Molecular Biology, The University of Ferrara, Ferrara, Italy;4. Department of Surgery, Li Ka Shing Medical Sciences Building, Prince of Wales Hospital, The Chinese University of Hong Kong, Hong Kong, People’s Republic of China;5. Department of Chemistry, Hong Kong Baptist University, Waterloo Road, Kowloon Tong, Hong Kong, People’s Republic of China |
| Abstract: | 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. |
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