Improved Synthesis and Structure-Activity Relationship of Coibamide A Analogues
Guiyang Yao; Wei Wang; Zhengyin Pan; Chunlei Wu; Lijing Fang; Wu Su
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
内容类型会议论文
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.
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