Design of β-carboline derivatives as DNA-targeting antitumor agents
Design of β-carboline derivatives as DNA-targeting antitumor agents
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DOI：
10.1016/j.ejmech.2006.05.004
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发表时间：
2006-10-01
影响因子：
6.7
通讯作者：
Xu, Anlong
中科院分区：
文献类型：
--
作者：
Guan, Huaji;Chen, Hongsheng;Xu, Anlong
This research studied the structure-activity relationship of beta-carboline derivatives as antitumor agents, in which 41 synthesized compounds and their cytotoxicity to tumor and normal cell lines were assayed. It was proved that substituent in position-9 of the beta-carboline ring could reinforce the DNA intercalating ability and consequently cytotoxicity to tumor cell lines, and the amidation of amino group at the end of the DNA targeting side chain in position-3 could cripple the DNA intercalating activity of these compounds, which resultingly initiated the cytotoxic selectivity to tumor cell lines rather than to normal ones. Furthermore, the S and G2-M arrest induced by these compounds confirmed that they could target DNA and lead to DNA destructions in Hela cells. In short, this study may provide a framework to design a novel antitumor drug that could surpass Adriamycin. (c) 2006 Elsevier Masson SAS. All rights reserved.
