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	Improved Total Synthesis and Biological Evaluation of Coibamide A Analogues
	Wu Su; Chunlei Wu; Lijing Fang; Guiyang Yao; Wei Wang
	2018
会议日期	2018
会议地点	深圳
英文摘要	Coibamide A is a highly potent antiproliferative cyclodepsipeptide originally isolated from a Panamanian marine cyanobacterium in 2007.[1] In our previous study, the first total synthesis and stereochemical revision of coibamide A were achieved. [3] 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, 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 optimizing the overall profile of coibamide A.
语种	英语
内容类型	会议论文
源URL	[http://ir.siat.ac.cn:8080/handle/172644/14741]
专题	深圳先进技术研究院_医药所
推荐引用方式 GB/T 7714	Wu Su,Chunlei Wu,Lijing Fang,et al. Improved Total Synthesis and Biological Evaluation of Coibamide A Analogues[C]. 见:. 深圳. 2018.

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