Structure-activity relationships of 1 '-acetoxychavicol acetate homologues as new nuclear export signal inhibitors

CORC > 南海海洋研究所 > 中国科学院南海海洋研究所 > 广东省应用海洋生物学重点实验室

	Structure-activity relationships of 1 '-acetoxychavicol acetate homologues as new nuclear export signal inhibitors
	Liu, Y ; Murakami, N ; Zhang, S ; Xu, T
刊名	PHARMAZIE
	2007
卷号	62 期号:9 页码:659
ISSN号	0031-7144
通讯作者	yonghongliu@scsio.ac.cn
合作状况	Bioassay-guided separation use of the fission yeast expressing NES of Rev, a HIV-1 viral regulatory protein, resulted in isolation of 1'-acetoxychavicol acetate (ACA) from Alpinia galanga as a new Rev-transport inhibitor from the nucleus to cytoplasm. Rational design and synthesis of eleven ACA derivatives containing systematic chemical variations were made, biological evaluation of inhibitory activities of these analogues provides the basis to formulate the structure-activity relationship (SAR). The key elements observed were: (1) The para substitution of the acetoxyl and 1'-acetoxypropenyl groups at the benzene ring was essential, (2) linear ethyl and propyl chain carbonates were more active than branching chain carbonates, (3) the substitution of acetoxyl groups with alkyl carbamate groups lost or reduced the activities. This study revealed a new salient pharmacophore features as potential drug leads against the HIV virus.
收录类别	662
原文出处	-
公开日期	2010-11-04 ; 2011-04-28
内容类型	期刊论文
源URL	[http://ir.scsio.ac.cn/handle/344004/1077]
专题	南海海洋研究所_广东省应用海洋生物学重点实验室
推荐引用方式 GB/T 7714	Liu, Y,Murakami, N,Zhang, S,et al. Structure-activity relationships of 1 '-acetoxychavicol acetate homologues as new nuclear export signal inhibitors[J]. PHARMAZIE,2007,62(9):659.
APA	Liu, Y,Murakami, N,Zhang, S,&Xu, T.(2007).Structure-activity relationships of 1 '-acetoxychavicol acetate homologues as new nuclear export signal inhibitors.PHARMAZIE,62(9),659.
MLA	Liu, Y,et al."Structure-activity relationships of 1 '-acetoxychavicol acetate homologues as new nuclear export signal inhibitors".PHARMAZIE 62.9(2007):659.