Design, synthesis and cytotoxic activity of novel spin-labeled camptothecin derivatives

摘要：

　　Continuing our search for natural product-based spin-labeled antitumor drugs,a series of novel spin-labeled camptothecin derivatives were synthesized via a Cu-catalyzed one pot reaction and evaluated for cytotoxicity against four tumor cell lines (A-549,MDA-MB-231,KB and KBvin).All target compounds (except for 9c and 9l) exhibited significant in vitro cytotoxic activity against the four tested tumor cell lines,notably against the drug resistant KBvin cancer cell line.Especially compounds 9e and 9j (IC50 0.0568 and 0.0720μM,respectively) displayed the greatest cytotoxicity against KBvin cancer cell line.Based on the observed cytotoxicity,preliminary structure–activity relationships have been described.

关键词： Camptothecin C-20 position spin labeled cytotoxic activity

作者: Mei-Juan Wang Kuo-Hsiung Lee Xiao-Bo Zhao Masuo Goto Susan L. Morris-Natschke Ying-Qian Liu Dan Wu Xiao-Bing Wu Zi-Long Song Gao-Xiang Zhu

作者单位: School of Pharmacy,Lanzhou University,Lanzhou 730000,PR China Natural Products Research Laboratories,UNC Eshelman School of Pharmacy,University of North Carolina, Natural Products Research Laboratories,UNC Eshelman School of Pharmacy,University of North Carolina,

会议类型: 国内会议

会议名称: 第十二届全国青年药学工作者最新科研成果交流会

会议地点: 南京

会议语种:英文

页码: 1-18

在线出版日期: 2014-06-10（万方平台首次上网日期，不代表论文的发表时间）