Synthesis and biological evaluation of bengacarboline derivatives

被引:18
作者
Pouilhes, Annie [1 ]
Kouklovsky, Cyrille [1 ]
Langlois, Yves [1 ]
Baltaze, Jean-Pierre [2 ]
Vispe, Stephane [3 ]
Annereau, Jean-Philippe [3 ]
Barret, Jean-Marc [3 ]
Kruczynski, Anna [3 ]
Bailly, Christian [3 ]
机构
[1] Univ Paris 11, ICMMO, UMR 8182, Lab Chim Procedes & Subst Nat, F-91405 Orsay, France
[2] Univ Paris 11, ICMMO, UMR 8182, Lab RMN Milieu Oriente, F-91405 Orsay, France
[3] Inst Rech Pierre Fabre, F-31432 Toulouse, France
关键词
bengacarboline; marine alakaloid; indole; cytotoxicity; DNA damages;
D O I
10.1016/j.bmcl.2007.11.113
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Novel derivatives of the marine alkaloid bengacarboline have been synthesized. The seco derivatives 11 and 12 were evaluated for topoisomerase inhibition, DNA damages, cytotoxicity and cell cycle perturbation. The two synthetic analogs are more potent cytotoxic agents than bengacarboline and they both induce an accumulation of cells in the S phase of DNA synthesis. They do not function as topoisomerase inhibitors but trigger DNA damages in cells. (C) 2008 Published by Elsevier Ltd.
引用
收藏
页码:1212 / 1216
页数:5
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