Synthesis, cytotoxicity and topoisomerase inhibition properties of multifarious aminoalkylated indeno[1,2-c]isoquinolin-5,11-diones

被引:12
作者
Ahn, Gang [1 ]
Schifano-Faux, Nadege [2 ]
Goossens, Jean-Francois [2 ]
Baldeyrou, Brigitte [3 ,4 ]
Couture, Axel [1 ]
Grandclaudon, Pierre [1 ,5 ]
Lansiaux, Amelie [3 ,4 ]
Ryckebusch, Adina [1 ,5 ]
机构
[1] Univ Lille 1, EA CMF 4478, F-59655 Villeneuve Dascq, France
[2] Univ Lille 2, EA 4481, Chim Analyt Lab, F-59006 Lille, France
[3] Univ Lille 2, Ctr Oscar Lambret, Inserm U837, IRCL, F-59045 Lille, France
[4] IMPRT, F-59045 Lille, France
[5] Ecole Natl Super Chim, F-59652 Villeneuve Dascq, France
关键词
Cancer; DNA intercalators; Topoisomerases; Indenoisoquinolines; I INHIBITORS; NITRATED INDENOISOQUINOLINES; ANTIPROLIFERATIVE EVALUATION; DNA INTERACTION; DERIVATIVES; RESISTANCE; OPTIMIZATION; ANHYDRIDES; ASSAYS;
D O I
10.1016/j.bmcl.2011.02.106
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A number of mono-or diaminoalkylated indeno[1,2-c]isoquinolin-5,11-diones analogs of 1 were synthesized and evaluated for their DNA binding affinities, topoisomerase inhibition properties and antiproliferative activities against human cancer cell lines (HL60). Impact of the side chain connected to the aromatic D ring and to the N6 lactam position on the biological profile will be discussed. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2259 / 2263
页数:5
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