Design, synthesis of symmetrical bivalent mimetics of annonaceous acetogenins and their cytotoxicities

被引:11
|
作者
Xiao, Qicai [2 ,3 ]
Liu, Yongqiang [4 ]
Qiu, Yatao [2 ]
Yao, Zhiyi [3 ]
Zhou, Guangbiao [4 ]
Yao, Zhu-Jun [1 ]
Jiang, Sheng [2 ]
机构
[1] Nanjing Univ, State Key Lab Coordinat Chem, Nanjing Natl Lab Microstruct, Sch Chem & Chem Engn, Nanjing 210093, Peoples R China
[2] Chinese Acad Sci, Lab Regenerat Biol, Guangzhou Inst Biomed & Hlth, Guangzhou 510530, Guangdong, Peoples R China
[3] Shanghai Inst Technol, Shanghai 210032, Peoples R China
[4] Chinese Acad Sci, Div Mol Carcinogenesis & Targeted Therapy Canc, State Key Lab Biomembrane & Membrane Biotechnol, Inst Zool, Beijing 100101, Peoples R China
关键词
Annonaceous acetogenins; Mimicry; Bivalent analogue; Cytotoxicity; Selectivity; REMARKABLE SELECTIVE CYTOTOXICITY; MIMICRY; ANALOGS; MECHANISMS; INDUCTION; STRATEGY; CANCER; CELLS;
D O I
10.1016/j.bmcl.2011.04.095
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A new series of linear dimeric compounds mimicking naturally occurring annonaceous acetogenins have been synthesized by bivalent analogue design, and their cytotoxicities have been evaluated against the growth of cancer cells by MTT method. Most of these compounds show selective action favored to human cancer cell lines over normal cell lines, and compound 9 with bis-terminal benzoquinone functionality exhibits an IC(50) = 0.40 mu M against MCF7 cell lines. This work mentions that appropriate conformational constraints might be a useful optimizing tool for this unique class of anticancer compounds. (C) 2011 Elsevier Ltd. All rights reserved.
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页码:3613 / 3615
页数:3
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