Synthesis of bufalin derivatives with inhibitory activity against prostate cancer cells

Yuan, Xiao-Feng and Tian, Hai-Yan and Li, Juan and Jin, Lu and Jiang, Shu-Tai and Liu, Ken Wing-Keung and Luo, Cheng and Middleton, David A. and Esmann, Mikael and Ye, Wen-Cai and Jiang, Ren-Wang (2014) Synthesis of bufalin derivatives with inhibitory activity against prostate cancer cells. Natural Product Research, 28 (11). pp. 843-847. ISSN 1478-6419

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Abstract

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.

Item Type:
Journal Article
Journal or Publication Title:
Natural Product Research
Uncontrolled Keywords:
/dk/atira/pure/subjectarea/asjc/1600/1602
Subjects:
ID Code:
72095
Deposited By:
Deposited On:
10 Dec 2014 09:03
Refereed?:
Yes
Published?:
Published
Last Modified:
22 Apr 2020 03:21