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学科主题: 生命有机化学
题名: Synthesis and anti-tumor activities of methyl 2-O-aryl-6-O-aryl '-D-glucopyranosides
其他题名: 具有抗癌活性的化合物甲基-2-氧-芳基-6-氧-芳基-D-Glucopyranosides的合成
作者: Shi HF(史合方) ; Zhou BC(周炳成) ; Li WW(李雯雯) ; Shi ZM(石志敏) ; Yu B(俞飚) ; Wang RX(王任小)
通讯作者: 俞飚 ; 王任小
刊名: Bioorg. Med. Chem. Lett.
发表日期: 2010
卷: 20, 期:9, 页:2855-2858
收录类别: SCI
部门归属: 中国科学院上海有机化学研究所; 中国海洋大学
英文摘要: A synthetic method of introducing bulky aryl groups at the 2-O- and 6-O-positions on glucopyranosides was developed. A total of 37 new compounds of this class were obtained successfully. These compounds were tested on several tumor cell lines by MTT assays, and some of them exhibited encouraging inhibitory activities. The most potent compound, CAB-SHZH-27, exhibited EC50 values of 14, 12, and 10 mu mol/L on A549, MDA-MB-231 and HeLa cells, respectively. A preliminary structure-activity relationship analysis indicates that the two free hydroxyl groups on the D-glucose core are indispensable for the biological activities of this class of compounds, and the aryl group at the 6-O-position has a more obvious impact than the one at the 2-O-position. An interesting 'on-off' mechanism of this class of compounds was also observed in our MTT assays, which remains to be explored. (C) 2010 Elsevier Ltd. All rights reserved.
语种: 英语
相关网址: 查看原文
WOS记录号: WOS:000276816600034
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/19123
Appears in Collections:生命有机化学国家重点实验室_期刊论文

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Recommended Citation:
Shi HF,Zhou BC,Li WW,et al. Synthesis and anti-tumor activities of methyl 2-O-aryl-6-O-aryl '-D-glucopyranosides[J]. Bioorg. Med. Chem. Lett.,2010,20(9):2855-2858.
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