| Novel synthetic acridine-based derivatives as topoisomerase Ⅰ inhibitors |
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| 作者姓名： | Bin Li Chun-Mei Gao Qin-Sheng Sun Lu-Lu Li Chun-Yan Tan Hong-Xia Liu Yu-Yang Jiang |
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| 作者单位： | a Tsinghua University, Department of Chemistry, Beijing 100084, China;b The Ministry-Province Jointly Constructed Base for State Key Lab-Shenzhen Key Laboratory of Chemical Biology, Shenzhen 518055, China;c Shenzhen Anti-Tumor Drug Development Engineering Laboratory, the Graduate School at Shenzhen, Tsinghua University, Shenzhen 518055, China;d School of Medicine, Tsinghua University, Beijing 100084, China |
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| 基金项目： | The authors would like to thank the Ministry of Science and Technology of the People＇s Republic of China （Nos. 2012AA020305 and 2011DFA30620）, the National Natural Science Foundation of China （Nos. 21272134 and 21372141）, and Shenzhen Sci. ＆ Tech. Bureau （No. JCYJ20120831165730905） for the financial supports. |
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| 摘 要： | Novel DNA binding agents against topoisomerases are needed for effective treatment of cancers. A series of new acridine-based derivatives 7a–7d were synthesized and their antiproliferative activity against K562 and HepG-2 cell lines were evaluated. Compound 7c with pyridin-2-yl-methanamino group substituted at the C9 position of acridine showed good antitumor activity against both cell lines. The DNA-binding affinity of compound 7c was evaluated by UV–vis absorption spectra and fluorescence emission spectra. DNA topoisomerase I mediated relaxation of plasmid pBR322 DNA was also tested. Our results suggested that compound 7c with good antitumor activity and topoisomerase I inhibition activity can be developed as a prime candidate for further chemical optimization.
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| 关 键 词： | 拓扑异构酶I 衍生物 吖啶 合成 抑制剂 抗肿瘤活性 K562细胞 荧光发射光谱 |
| 收稿时间： | 2013-12-25 |
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