Synthesis and biological evaluation of bufalin-3-yl nitrogen-containing-carbamate derivatives as anticancer agents
文献类型：期刊论文
| 作者 | Lei, Min1,2 ; Xiao, Zhiyong1; Ma, Biao1; Chen, Yijia1; Liu, Miao1; Liu, Junhua1,2; Guo, De'an1; Liu, Xuan1; Hu, Lihong1
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| 刊名 | STEROIDS
 |
| 出版日期 | 2016-04 |
| 卷号 | 108页码:56-60 |
| 关键词 | Cardiac glycosides Bufalin (BF) Natural product Bufalin-3-yl carbamate Cytotoxicity |
| ISSN号 | 0039-128X |
| DOI | 10.1016/j.steroids.2016.01.011 |
| 文献子类 | Article |
| 英文摘要 | A series of bufalin-3-yl nitrogen-containing-carbamate derivatives 3 were designed, synthesized, and evaluated for their proliferation inhibition activities against human cervical epithelial adenocarcinoma (HeLa) cell line. The structure-activity relationships (SARs) of this new series are described in this paper. Cytotoxicity data revealed that the C3 moiety had an important influence on cytotoxic activity. Compound 3i-HCl exhibited significant in vitro antiproliferative activity against the ten tested tumor cell lines, with IC50 values ranging from 0.30 to 1.09 nM. Furthermore, 3i-HCl can significantly inhibit tumor growth by 100% at the dose 2 mg/kg by iv, or 4 mg/kg by ig. (C) 2016 Elsevier Inc. All rights reserved. |
| WOS关键词 | MADAGASCAR RAIN-FOREST ; CARDENOLIDE GLYCOSIDES ; CARDIAC-GLYCOSIDES ; CANCER CELLS ; BUFADIENOLIDES ; CYTOTOXICITY |
| 资助项目 | Chinese National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2013ZX09508104] ; Chinese National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2014ZX09301-306-003] ; Open Project Program of State Key Laboratory of Natural Medicines, China Pharmaceutical University[SKLNMKF201413] ; Shanghai Science & Technology Support Program[13431900401] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Endocrinology & Metabolism |
| 语种 | 英语 |
| WOS记录号 | WOS:000373648700007 |
| 出版者 | ELSEVIER SCIENCE INC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276094]  |
| 专题 | 上海中药现代化研究中心 |
| 通讯作者 | Lei, Min |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Res Ctr Modernizat Tradit Chinese Med, Shanghai 201203, Peoples R China; 2.China Pharmaceut Univ, State Key Lab Nat Med, Nanjing 210009, Jiangsu, Peoples R China |
| 推荐引用方式 GB/T 7714 | Lei, Min,Xiao, Zhiyong,Ma, Biao,et al. Synthesis and biological evaluation of bufalin-3-yl nitrogen-containing-carbamate derivatives as anticancer agents[J]. STEROIDS,2016,108:56-60. |
| APA | Lei, Min.,Xiao, Zhiyong.,Ma, Biao.,Chen, Yijia.,Liu, Miao.,...&Hu, Lihong.(2016).Synthesis and biological evaluation of bufalin-3-yl nitrogen-containing-carbamate derivatives as anticancer agents.STEROIDS,108,56-60. |
| MLA | Lei, Min,et al."Synthesis and biological evaluation of bufalin-3-yl nitrogen-containing-carbamate derivatives as anticancer agents".STEROIDS 108(2016):56-60. |
入库方式： OAI收割
来源：上海药物研究所
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