Structure-activity relationships of 1 '-acetoxychavicol acetate homologues as new nuclear export signal inhibitors
Liu, Y; Murakami, N; Zhang, S; Xu, T; yonghongliu@scsio.ac.cn
2007
发表期刊PHARMAZIE
ISSN0031-7144
卷号62期号:9页码:659-662
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.
部门归属Chinese Acad Sci, S China Sea Inst Oceanol, Ky Lab Marine Bioresources Sustainable Utilizat, Guangzhou 510301, Peoples R China
学科领域Chemistry, Medicinal ; Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
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收录类别sci
资助项目LMB
WOS记录号WOS:000249943200002
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被引频次:5[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.scsio.ac.cn/handle/344004/4914
专题中科院海洋生物资源可持续利用重点实验室
通讯作者yonghongliu@scsio.ac.cn
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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):659-662.
APA Liu, Y,Murakami, N,Zhang, S,Xu, T,&yonghongliu@scsio.ac.cn.(2007).Structure-activity relationships of 1 '-acetoxychavicol acetate homologues as new nuclear export signal inhibitors.PHARMAZIE,62(9),659-662.
MLA Liu, Y,et al."Structure-activity relationships of 1 '-acetoxychavicol acetate homologues as new nuclear export signal inhibitors".PHARMAZIE 62.9(2007):659-662.
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