Structure-activity relationships of diverse annonaceous acetogenins against human tumor cells

被引:29
作者
Yang, Haijun [1 ]
Zhang, Ning [1 ]
Li, Xiang [1 ]
Chen, Jianwei [1 ]
Cai, Baochang [2 ]
机构
[1] Nanjing Univ Chinese Med, Dept Pharm, Nanjing 210046, Peoples R China
[2] Nanjing Univ Chinese Med, Key Proc Lab Jangsu, Nanjing 210046, Peoples R China
关键词
Annonace; Annonaceous acetogenins; Structure-activity relationship; Cytotoxicities; MITOCHONDRIAL COMPLEX-I; POTENT INHIBITORS; BULLATACIN; ANTITUMOR; ANALOGS; MODE;
D O I
10.1016/j.bmcl.2009.02.105
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Twelve annonaceous acetogenins (ACGs) with different stereochemical structures and configuration were selected to test for their inhibitions on the growth of Hela, SMMC-7541, SGC-7901, MCF-7 and A-5408 tumor cell lines using MTT method. This was the first to simultaneously investigate effects of structural factors of stereochemical structures and configuration on cytotoxicities with structure-activity relationship. The present study showed that cytotoxic selectivities of ACGs with threo/trans/threo/trans/erythro stereochemical arrangement were gently more active than those with threo/trans/threo/trans/threo stereochemical arrangement, and ACGs with cis THF ring partly produced notable cytotoxic selectivities. Furthermore, ACGs with S configuration at C-24 exhibited gently more cytotoxic selectivities potency than those with R configuration at C-24. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2199 / 2202
页数:4
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