Synthesis and antiproliferative activity of 9-benzylamino-6-chloro-2-methoxy-acridine derivatives as potent DNA-binding ligands and topoisomerase II inhibitors
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- 作者：Wei Zhanga ; b ; c ; Bin Zhangc ; Wei Zhangb ; c ; Ti Yanga ; Ning Wanga ; b ; Chunmei Gaoa ; b ; chunmeigao@sz.tsinghua.edu.cn" class="auth_mail" title="E-mail the corresponding author ; Chunyan Tanb ; d ; Hongxia Liub ; Yuyang Jianga ; b ; d ; jiangyy@sz.tsinghua.edu.cn" class="auth_mail" title="E-mail the corresponding author
- 关键词：Acridine derivatives ; Topoisomerase II inhibitor ; Antiproliferative activity ; DNA damage
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：30 June 2016
- 年：2016
- 卷：116
- 期：Complete
- 页码：59-70
- 全文大小：1997 K
文摘
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A series of 9-benzylamino acridines were synthesized.
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The in vitro cytotoxic effects in cancer cells were evaluated.
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Compound 8p acted as a potent DNA-binding Ligand and topoisomerase II inhibitor.
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Compound 8p induced a potent apoptotic response in A549 lung cancer cells.
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Compound 8p arrested A549 lung cancer cells at the G2/M-phase.