Synthesis and structure-activity relationships study of cytotoxic bufalin 3-nitrogen-containing-ester derivatives
文献类型：期刊论文
| 作者 | Ma, Biao; Xiao, Zhi-Yong; Chen, Yi-Jia; Lei, Min ; Meng, Yu-Hui; Guo, De-An; Liu, Xuan; Hu, Li-Hong
|
| 刊名 | STEROIDS
 |
| 出版日期 | 2013-05 |
| 卷号 | 78期号:5页码:508-512 |
| 关键词 | Bufalin Bufalin 3-nitrogen-containing-ester Structure-activity relationships Cytotoxicity |
| ISSN号 | 0039-128X |
| DOI | 10.1016/j.steroids.2013.02.007 |
| 文献子类 | Article |
| 英文摘要 | A series of bufalin 3-nitrogen-containing-ester derivatives (2-6) were designed, synthesized, and evaluated for their proliferation inhibition activities against human cervical epithelial adenocarcinoma (HeLa) and non-small-cell lung cancer (A549) cell lines. The structure-activity relationships (SARs) of this new series were described in this paper. Cytotoxicity data revealed that C3 moiety had important influence on cytotoxic activity. On two cell lines, the bufalin-3-piperidinyl-4-carboxylate compound 2 (IC50 values on HeLa and A549 cell lines were 0.76 nM and 0.34 nM, respectively) displayed a significant cytotoxic potency compared to the parent compound bufalin. (C) 2013 Elsevier Inc. All rights reserved. |
| WOS关键词 | CHAN-SU ; BUFADIENOLIDES ; CARCINOMA ; APOPTOSIS ; CELLS |
| 资助项目 | National Natural Science Foundation of China[30925040] ; National Natural Science Foundation of China[81102329] ; Chinese National Science 82 Technology Major Project "Key New Drug Creation and Manufacturing Program"[2012ZX09301001-001] ; Chinese National Science 82 Technology Major Project "Key New Drug Creation and Manufacturing Program"[2011ZX09307-002-03] ; Science Foundation of Shanghai[12XD14057] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Endocrinology & Metabolism |
| 语种 | 英语 |
| WOS记录号 | WOS:000318385700009 |
| 出版者 | ELSEVIER SCIENCE INC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277639]  |
| 专题 | 上海中药现代化研究中心 |
| 通讯作者 | Liu, Xuan |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Res Ctr Modernizat Tradit Chinese Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ma, Biao,Xiao, Zhi-Yong,Chen, Yi-Jia,et al. Synthesis and structure-activity relationships study of cytotoxic bufalin 3-nitrogen-containing-ester derivatives[J]. STEROIDS,2013,78(5):508-512. |
| APA | Ma, Biao.,Xiao, Zhi-Yong.,Chen, Yi-Jia.,Lei, Min.,Meng, Yu-Hui.,...&Hu, Li-Hong.(2013).Synthesis and structure-activity relationships study of cytotoxic bufalin 3-nitrogen-containing-ester derivatives.STEROIDS,78(5),508-512. |
| MLA | Ma, Biao,et al."Synthesis and structure-activity relationships study of cytotoxic bufalin 3-nitrogen-containing-ester derivatives".STEROIDS 78.5(2013):508-512. |
入库方式： OAI收割
来源：上海药物研究所
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