Synthesis and cytotoxicity evaluation of 4 '-amino-4 '-dehydroxyloleandrin derivatives
文献类型：期刊论文
| 作者 | Chen, Hu1; Lei, Min2 ; Ma, Biao2; Liu, Miao2; Guo, Dean2; Liu, Xuan2; Hu, Lihong1,2
|
| 刊名 | FITOTERAPIA
 |
| 出版日期 | 2016-09 |
| 卷号 | 113页码:85-90 |
| 关键词 | Oleandrin Antitumor agent Natural product Cytotoxicity Structure-activity relationships (SARs) |
| ISSN号 | 0367-326X |
| DOI | 10.1016/j.fitote.2016.07.002 |
| 文献子类 | Article |
| 英文摘要 | A series of C4'-substituted oleandrin analogues were designed, synthesized and evaluated for their cytotoxicity towards human cervical carcinoma cell line (HeLa). The structure-activity relationships (SARs) of these compounds were summarized in this paper, and 4'-alpha-amino-4'-dehydroxyloleandrin 4a (IC50 = 21.7 nM) and 4'-beta-amino-4'-dehydroxyloleandrin 4b (IC50 = 10.9 nM) exhibited stronger cytotoxicity compared with oleandrin (IC50 = 33.3 nM). Furthermore, the cytotoxicity of these two compounds towards another five human cancer cell lines (NCI-H266, A549, Jurkat, HL-60 and PC-3) was also evaluated and the IC50 values of beta-amino derivative 4b were approximately 2-3 folds lower than that of oleandrin. (C) 2016 Published by Elsevier B.V. |
| WOS关键词 | MADAGASCAR RAIN-FOREST ; CARDIAC-GLYCOSIDES ; CARDENOLIDE GLYCOSIDES ; CELL-DEATH ; POTENTIATES APOPTOSIS ; NERIUM-OLEANDER ; CANCER-CELLS ; SOLID TUMORS ; ACTIVATION ; EXPRESSION |
| 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"[2014ZX09301306-003] ; Shanghai Science & Technology Support Program[13431900401] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000383301200012 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275912]  |
| 专题 | 上海中药现代化研究中心 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 | Lei, Min; Liu, Xuan; Hu, Lihong |
| 作者单位 | 1.East China Univ Sci & Technol, Shanghai Key Lab New Drug Design, Sch Pharm, Shanghai 200237, Peoples R China; 2.Chinese Acad Sci, Univ Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Chen, Hu,Lei, Min,Ma, Biao,et al. Synthesis and cytotoxicity evaluation of 4 '-amino-4 '-dehydroxyloleandrin derivatives[J]. FITOTERAPIA,2016,113:85-90. |
| APA | Chen, Hu.,Lei, Min.,Ma, Biao.,Liu, Miao.,Guo, Dean.,...&Hu, Lihong.(2016).Synthesis and cytotoxicity evaluation of 4 '-amino-4 '-dehydroxyloleandrin derivatives.FITOTERAPIA,113,85-90. |
| MLA | Chen, Hu,et al."Synthesis and cytotoxicity evaluation of 4 '-amino-4 '-dehydroxyloleandrin derivatives".FITOTERAPIA 113(2016):85-90. |
入库方式： OAI收割
来源：上海药物研究所
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