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Antitumor activity of diethynylfluorene derivatives of gold(I).

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.
AuthorsChung-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
JournalBioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 17 Issue 23 Pg. 7872-7 (Dec 01 2009) ISSN: 1464-3391 [Electronic] England
PMID19889546 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents
  • Fluorenes
  • Organometallic Compounds
  • Gold
Topics
  • Animals
  • Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
  • Cell Line, Tumor
  • Cell Survival (drug effects)
  • Fluorenes (chemical synthesis, chemistry, pharmacology)
  • Gold (chemistry, pharmacology)
  • Humans
  • Magnetic Resonance Spectroscopy
  • Mice
  • Mice, Nude
  • Neoplasms, Experimental (drug therapy)
  • Organometallic Compounds (chemistry, pharmacology)
  • Spectrometry, Mass, Fast Atom Bombardment
  • Spectroscopy, Fourier Transform Infrared
  • Structure-Activity Relationship

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