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SCSIO OpenIR  > 广东省应用海洋生物学重点实验室  > 期刊论文
题名: Structure-activity relationships of 1 '-acetoxychavicol acetate homologues as new nuclear export signal inhibitors
作者: Liu, Y ; Murakami, N ; Zhang, S ; Xu, T
通讯作者: yonghongliu@scsio.ac.cn
刊名: PHARMAZIE
发表日期: 2007
卷: 62, 期:9, 页:659
收录类别: 662
合作性质: 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.
部门归属: LMB
产权排名: CONCATENATE(P24,Q24,R24)
原文出处: 查看原文
内容类型: 期刊论文
URI标识: http://ir.scsio.ac.cn/handle/344004/1077
Appears in Collections:广东省应用海洋生物学重点实验室_期刊论文

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Recommended Citation:
Liu, Y; Murakami, N; Zhang, S; Xu, T.Structure-activity relationships of 1 '-acetoxychavicol acetate homologues as new nuclear export signal inhibitors,PHARMAZIE,2007,62(9):659
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