Synthesis and biochemical properties of E-ring modified luotonin A derivatives

被引:48
作者
Cagir, A
Jones, SH
Eisenhauer, BM
Gao, R
Hecht, SM
机构
[1] Univ Virginia, Dept Chem, Charlottesville, VA 22901 USA
[2] Univ Virginia, Dept Biol, Charlottesville, VA 22901 USA
关键词
topoisomerase I poisons; antineoplastic agents; cytotoxic alkaloids;
D O I
10.1016/j.bmcl.2004.02.069
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Luotonin A is a cytotoxic pyrroloquinazolinoquinoline alkaloid that has been shown to stabilize the human topoisomerase I-DNA covalent binary complex in the same fashion Lis the antitumor alkaloid camptothecin. A study of the structural elements in luotonin A required for binary complex stabilization has revealed key differences relative to those required for camptothecin. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2051 / 2054
页数:4
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