Synthesis and structure-activity relationship studies of cytotoxic cinnamic alcohol derivatives

被引:6
|
作者
Zou, Hong-Bin [1 ,2 ]
Zhang, Liang [1 ]
Yang, Lei-Xiang [1 ]
Yang, Liu-Qing [1 ,2 ]
Zhao, Yu [1 ]
Yu, Yong-Ping [1 ]
Stoeckigt, Joachim [1 ,2 ]
机构
[1] Zhejiang Univ, Inst Mat Med, Coll Pharmaceut Sci, Hangzhou 310058, Zhejiang, Peoples R China
[2] Johannes Gutenberg Univ Mainz, Lehrstuhl Pharmazeut Biol, Inst Pharm, D-55099 Mainz, Germany
关键词
cinnamic alcohol derivatives; cytotoxicity; structure-activity relationship; SINAPYL ALCOHOL; SYRINGIN;
D O I
10.1080/14786410902830175
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
Three series of di- and trisubstituted derivatives of cinnamic alcohol and its conjugated dienol analogues were designed and synthesised. The derivatives were screened for cytotoxicity against nine tumour cell lines: KB, A549, Hela, CNE, PC-3, BEL-7404, HL-60, BGC823 and P388D1. Most of the cinnamic alcohol derivatives showed cytotoxic activity. The compound 7-(4',5'-dichlorobenzyloxy)-6,8-dihydroxycinnamic alcohol (55) exhibited significant cytotoxicity to seven human tumour cell lines on a micromolar range, especially with regard to the KB and P388D1 cell lines, showing IC50 values of 0.4 and 0.5 mu M, respectively. The structure-activity relationships of the derivatives are discussed.
引用
收藏
页码:203 / 221
页数:19
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