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A convenient way to synthesize bufadienolactam analogs with inhibitory activity against the prostate cancer cells
Xiao-Feng Yuan 1,Hai-Yan Tian 2,Juan Li 2 #,Shu-Tai Jiang 2,Ken Wing-Keung Liu 3,David A. Middleton 4,Wen-Cai Ye 2,Ren-Wang Jiang 2 *
1.Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou 510632
2.Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou 510632, P. R. China.
3.School of Biomedical Sciences, The Chinese University of Hong Kong, Shatin, Hong Kong SAR, P. R. China.
4.Department of Structural Biology, School of Biological Sciences, University of Liverpool, Crown Street, Liverpool L69 7ZQ, U.K.
*Correspondence author
#Submitted by
Subject:
Funding: National Natural Science Foundation of China (No.81102518), the Fundamental Research Funds for the Central Universities (No.11612603), Postdoctoral Granted Financial Support (No.20110490915)
Opened online: 7 March 2013
Accepted by: none
Citation: Xiao-Feng Yuan,Hai-Yan Tian,Juan Li.A convenient way to synthesize bufadienolactam analogs with inhibitory activity against the prostate cancer cells[OL]. [ 7 March 2013] http://en.paper.edu.cn/en_releasepaper/content/4525029
 
 
Bufadienolactam (1) and secobufalinamide (2) were synthesized by treatment of bufalin with ammonium acetate in DMF solution. Their structures were elucidated by extensive spectroscopic methods. The structure of 2 was further confirmed by single-crystal X-ray diffraction analysis. Compound 1 and 2 didn't inhibit the Na+/K+-ATPase. However, both compounds showed significant inhibitory activity against the androgen dependent prostate cell LNCaP with IC50 values of 9.0 μM for 1 and 14.0μM for 2. The fact that compounds 1 and 2 inhibited the prostate cancer cells but no inhibition on Na+/K+-ATPase indicated that they might be potential anti-prostate cancer agents without the cardiac toxicity.
Keywords:prostate cancer; bufalin; Na+/K+-ATPase
 
 
 

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