Antitumor activity of diethynylfluorene derivatives of gold(I)
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- 作者：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
- 关键词：Alkynes ; Fluorenes derivatives ; Gold(I) complexes ; Human carcinoma cells ; Nude mice model ; Reactive oxygen species
- 刊名：Bioorganic and Medicinal Chemistry
- 出版年：2009
- 出版时间：1 December 2009
- 年：2009
- 卷：17
- 期：23
- 页码：7872-7877
- 全文大小：458 K
文摘
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.