李晓莲

个人信息Personal Information

教授

硕士生导师

性别:女

毕业院校:大连理工大学

学位:博士

所在单位:化工学院

学科:应用化学. 精细化工. 有机化学

办公地点:化工实验楼E座514

联系方式:0411-84986324 13504280675

电子邮箱:xlianli@dlut.edu.cn

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The novel anti-tumor agents of 4-triazol-1,8-naphthalimides: Synthesis, cytotoxicity, DNA intercalation and photocleavage

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论文类型:期刊论文

发表时间:2011-04-01

发表刊物:EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

收录刊物:Scopus、SCIE、PubMed

卷号:46

期号:4

页面范围:1274-1279

ISSN号:0223-5234

关键字:Triazole; Intercalation; Anticancer; Naphthalimides

摘要:A novel series of 4-(4-phenyl-[1,2,3]-triazol-1-yl)-1,8-naphthalimide derivatives had been synthesized easily by employing "click reaction". For anti-tumor activity in vitro, all the compounds were found to be more toxic against MCF-7 than Hela and 7721 cells. 4a, 4b and 4e Showed improved cytotoxic activity against MCF-7 cells over Amonafide, in particular compound 4a, with an IC(50) could amount to 10(-7) M. The UV-vis spectra and Circular Dichroism titration indicated that the compounds behaved as effective DNA-intercalating agents. The investigation of their photo-damaging ability illuminated that these compounds could damage DNA effectively into form II and even form III. (c) 2011 Elsevier Masson SAS. All rights reserved.