Antitumor agents. 266. Design, synthesis, and biological evaluation of novel 2-(furan-2-yl)naphthalen-1-ol derivatives as potent and selective antibreast cancer agents

  • J Med Chem. 2009 Jun 11;52(11):3586-90. doi: 10.1021/jm9001567.
Yizhou Dong  1 ,  Qian Shi ,  Yi-Nan Liu ,  Xiang Wang ,  Kenneth F Bastow ,  Kuo-Hsiung Lee
Affiliations
  • 1. Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA.
PMID: 19425534 DOI: 10.1021/jm9001567
Abstract

In a continuing study, we explored how the individual rings in neo-tanshinlactone (1) influence its potent and selective in vitro antibreast Cancer activity. Accordingly, we discovered a novel class of antibreast Cancer agents, 2-(furan-2-yl)naphthalen-1-ol derivatives, based on an active C-ring opened model compound 5. Further optimization led to 18 and 21, which showed decreased cytotoxic potency but better selectivity than neo-tanshinlactone analogue 2. Interestingly, 20 showed broad cytotoxicity against human Cancer cell lines.