Improved Total Synthesis and Biological Evaluation of Coibamide A Analogues
文献类型：期刊论文
| 作者 | Liu, Ke; Yao, Guiyang; Wang, Wei; Ao, Lijiao; Cheng, Zhehong; Wu, Chunlei; Pang, Zhengyin; Li, Hongchang; Su, Wu; Fang, Lijing |
| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2018 |
| 文献子类 | 期刊论文 |
| 英文摘要 | To enable the large-scale synthesis of coibamide A, we developed an improved synthetic strategy for this class of cyclodepsipeptide. The versatility of the synthetic procedure was demonstrated by the preparation of a series of designed coibamide A analogues, which enabled the preliminary structure-activity relationship (SAR) studies for this compound. Although most modifications of coibamide A resulted in decrease or loss of the antiproliferativity, we found that versatile substitution at position 3 was well tolerated. Remarkably, a simplified analogue, [MeAla3-MeAla6]-coibamide (1f), not only showed nearly the same inhibition as coibamide A against the tested cancer cells but also significantly inhibited tumor growth in vivo. The improved synthetic strategy and the relevant trends of SAR disclosed in this study will be valuable for further optimization of the overall profile of coibamide A. |
| URL标识 | 查看原文 |
| 语种 | 英语 |
| 源URL | [http://ir.siat.ac.cn:8080/handle/172644/14615]  |
| 专题 | 深圳先进技术研究院_医药所 |
| 推荐引用方式 GB/T 7714 | Liu, Ke,Yao, Guiyang,Wang, Wei,et al. Improved Total Synthesis and Biological Evaluation of Coibamide A Analogues[J]. JOURNAL OF MEDICINAL CHEMISTRY,2018. |
| APA | Liu, Ke.,Yao, Guiyang.,Wang, Wei.,Ao, Lijiao.,Cheng, Zhehong.,...&Fang, Lijing.(2018).Improved Total Synthesis and Biological Evaluation of Coibamide A Analogues.JOURNAL OF MEDICINAL CHEMISTRY. |
| MLA | Liu, Ke,et al."Improved Total Synthesis and Biological Evaluation of Coibamide A Analogues".JOURNAL OF MEDICINAL CHEMISTRY (2018). |
入库方式： OAI收割
来源：深圳先进技术研究院
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。