Improved Total Synthesis and Biological Evaluation of Coibamide A Analogues

	Improved Total Synthesis and Biological Evaluation of Coibamide A Analogues
	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
	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
内容类型	期刊论文
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).