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Synthesis of bufalin derivatives with inhibitory activity against prostate cancer cells

Research output: Contribution to Journal/MagazineJournal articlepeer-review

  • Xiao-Feng Yuan
  • Hai-Yan Tian
  • Juan Li
  • Lu Jin
  • Shu-Tai Jiang
  • Ken Wing-Keung Liu
  • Cheng Luo
  • David A. Middleton
  • Mikael Esmann
  • Wen-Cai Ye
  • Ren-Wang Jiang
<mark>Journal publication date</mark>3/06/2014
<mark>Journal</mark>Natural Product Research
Issue number11
Number of pages5
Pages (from-to)843-847
Publication StatusPublished
<mark>Original language</mark>English


Bufalin possesses a strong anti-cancer effect, but the cardiac toxicity targeting the Na+, K+-ATPase limits its application. Here, two bufalin derivatives, bufadienolactam (1) and secobufalinamide (2), were synthesised by treating bufalin with ammonium acetate in dimethylformamide solution. Their structures were elucidated by extensive spectroscopic methods. The structure of compound 2 was further confirmed by single-crystal X-ray diffraction analysis. Compounds 1 and 2 expressed strong inhibitory activities against androgen-dependent prostate cancer cells (IC50 values about 10 mu M), but only weak inhibition on Na+, K+-ATPase (K-i about 70 mu M), indicating that they might be potential anti-prostate cancer agents without severe cardiac toxicity.