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学科主题: Chemistry, Medicinal; Chemistry, Multidisciplinary; Pharmacology & Pharmacy
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:659-662
收录类别: sci
部门归属: Chinese Acad Sci, S China Sea Inst Oceanol, Ky Lab Marine Bioresources Sustainable Utilizat, Guangzhou 510301, Peoples R China
项目归属: LMB
摘要: 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.
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WOS记录号: WOS:000249943200002
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内容类型: 期刊论文
URI标识: http://ir.scsio.ac.cn/handle/344004/4914
Appears in Collections:中科院海洋生物资源可持续利用重点实验室_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):659-662
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