Design, synthesis and anti-tumor activities of carbamate derivatives of cinobufagin
文献类型：期刊论文
| 作者 | Zhou, Yang1,2; Hou, Jinjun1,2 ; Long, Huali1,2; Zhang, Zijia1,2; Lei, Min1,2; Wu, Wanying1,2
|
| 刊名 | STEROIDS
 |
| 出版日期 | 2020-12-01 |
| 卷号 | 164页码:11 |
| 关键词 | Cardiac glycosides Cinobufagin Natural product Cytotoxicity Antiproliferative activities |
| ISSN号 | 0039-128X |
| DOI | 10.1016/j.steroids.2020.108749 |
| 通讯作者 | Lei, Min(mlei@simm.ac.cn) ; Wu, Wanying(wanyingwu@simm.ac.cn) |
| 英文摘要 | A series of cinobufagin-3-yl nitrogen-containing-carbamate derivatives were designed, synthesized, and evalu-ated for their proliferation inhibition activities. The structure-activity relationships suggested that the substituents at C-16 was a crucial factor for the potency and that follows this trends: acetic ester >> benzoic ester approximate to hydroxy > carbamate. Compounds 3f, 3g, 3h, and 3i exhibited significant in vitro antiproliferative activities against the eight tested tumor cell lines, with IC50 values ranging from 8.1 to 237.4 nM. Furthermore, 3g tartrate (3g-TA) significantly inhibited tumor growth by 64.5%, 83.9%, and 93.0% at a doses of 4, 6, 8 mg/kg/qod by ip, respectively. |
| WOS关键词 | CARDIAC-GLYCOSIDES ; CARDENOLIDE GLYCOSIDES ; BUFADIENOLIDES ; CYTOTOXICITY |
| 资助项目 | Special Fund for Strategic Pilot Technology Chinese Academy of Sciences[XDA12020379] ; National Natural Science Foundation of China[81973455] ; National Key R&D Program of China[2018YFC1707900] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Endocrinology & Metabolism |
| 语种 | 英语 |
| WOS记录号 | WOS:000592420700009 |
| 出版者 | ELSEVIER SCIENCE INC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/296217]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Lei, Min; Wu, Wanying |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Res Ctr Modernizat Tradit Chinese Med, Shanghai Inst Mat Med, Natl Engn Lab TCM Standardizat Technol, Shanghai 201203, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhou, Yang,Hou, Jinjun,Long, Huali,et al. Design, synthesis and anti-tumor activities of carbamate derivatives of cinobufagin[J]. STEROIDS,2020,164:11. |
| APA | Zhou, Yang,Hou, Jinjun,Long, Huali,Zhang, Zijia,Lei, Min,&Wu, Wanying.(2020).Design, synthesis and anti-tumor activities of carbamate derivatives of cinobufagin.STEROIDS,164,11. |
| MLA | Zhou, Yang,et al."Design, synthesis and anti-tumor activities of carbamate derivatives of cinobufagin".STEROIDS 164(2020):11. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。