Synthesis of bufalin derivatives with inhibitory activity against prostate cancer cells
文献类型：期刊论文
| 作者 | Yuan, Xiao-Feng1; Tian, Hai-Yan1; Li, Juan1; Jin, Lu1,2; Jiang, Shu-Tai1; Liu, Ken Wing-Keung3; Luo, Cheng2 ; Middleton, David A.4; Esmann, Mikael5; Ye, Wen-Cai1
|
| 刊名 | NATURAL PRODUCT RESEARCH
 |
| 出版日期 | 2014-06-03 |
| 卷号 | 28期号:11页码:843-847 |
| 关键词 | bufalin prostate cancer Na+ K+-ATPase androgen receptor |
| ISSN号 | 1478-6419 |
| DOI | 10.1080/14786419.2014.881363 |
| 文献子类 | Article |
| 英文摘要 | 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. |
| WOS关键词 | ANDROGEN-RECEPTOR-ANTAGONIST ; THERAPY |
| 资助项目 | Guangdong High Level Talent Scheme[00000000] ; National Natural Science Foundation of China[81102518] ; National Major Scientific Program of Introducing Talents of Discipline to Universities[B13038] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000335942400002 |
| 出版者 | TAYLOR & FRANCIS LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277035]  |
| 专题 | 药物发现与设计中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Jiang, Ren-Wang |
| 作者单位 | 1.Jinan Univ, Coll Pharm, Guangdong Prov Key Lab Pharmacodynam Constituents, Guangzhou 510632, Guangdong, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 3.Chinese Univ Hong Kong, Sch Biomed Sci, Shatin, Hong Kong, Peoples R China; 4.Univ Liverpool, Inst Integrat Biol, Liverpool L69 7ZQ, Merseyside, England; 5.Aarhus Univ, Dept Biomed, DK-8000 Aarhus, Denmark |
| 推荐引用方式 GB/T 7714 | Yuan, Xiao-Feng,Tian, Hai-Yan,Li, Juan,et al. Synthesis of bufalin derivatives with inhibitory activity against prostate cancer cells[J]. NATURAL PRODUCT RESEARCH,2014,28(11):843-847. |
| APA | Yuan, Xiao-Feng.,Tian, Hai-Yan.,Li, Juan.,Jin, Lu.,Jiang, Shu-Tai.,...&Jiang, Ren-Wang.(2014).Synthesis of bufalin derivatives with inhibitory activity against prostate cancer cells.NATURAL PRODUCT RESEARCH,28(11),843-847. |
| MLA | Yuan, Xiao-Feng,et al."Synthesis of bufalin derivatives with inhibitory activity against prostate cancer cells".NATURAL PRODUCT RESEARCH 28.11(2014):843-847. |
入库方式： OAI收割
来源：上海药物研究所
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