Improved Synthesis and Structure-Activity Relationship of Coibamide A Analogues
文献类型：会议论文
| 作者 | Guiyang Yao; Wei Wang; Zhengyin Pan; Chunlei Wu; Lijing Fang; Wu Su |
| 出版日期 | 2016 |
| 会议名称 | CPS2016(The 14th Chinese International Peptide Symposium & the 5th Asia-pacific International Peptide Symposium) |
| 会议地点 | 中国南京 |
| 英文摘要 | Coibamide A is a highly potent antiproliferative cyclodepsipeptide originally isolated from a Panamanian marine cyanobacterium in 2007[1-2]. In our previous study, the first total synthesis and stereochemical revision of coibamide A were achieved[3]. Herein we report an improved solid-phase strategy for assembly of coibamide A analogues and their in vitro activity on a panel of human cancer cell lines. The structure-activity relationship of these analogues revealed that coibamide A is highly sensitive to backbone stereotopical modification but not to side chain size modification. These observations suggest that this compound has a defined conformational structure and also that it interacts with chiral compounds through its backbone and not through its side chains. Based on these results, biotin-labeled analogues are designed to elucidate the unknown mode of action of coibamide A. |
| 收录类别 | 其他 |
| 语种 | 英语 |
| 源URL | [http://ir.siat.ac.cn:8080/handle/172644/10818]  |
| 专题 | 深圳先进技术研究院_医药所 |
| 作者单位 | 2016 |
| 推荐引用方式 GB/T 7714 | Guiyang Yao,Wei Wang,Zhengyin Pan,et al. Improved Synthesis and Structure-Activity Relationship of Coibamide A Analogues[C]. 见:CPS2016(The 14th Chinese International Peptide Symposium & the 5th Asia-pacific International Peptide Symposium). 中国南京. |
入库方式： OAI收割
来源：深圳先进技术研究院
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