Synthesis and biological evaluation of new dipyrrolo[3,4-a:3,4-c]carbazole-1,3,4,6-tetraones, substituted with various saturated and unsaturated side chains via palladium catalyzed cross-coupling reactions

被引:24
作者
Henon, Helene
Anizon, Fabrice
Golsteyn, Roy M.
Leonce, Stephane
Hofmann, Robert
Pfeiffer, Bruno
Prudhomme, Michelle [1 ]
机构
[1] Univ Clermont Ferrand, Lab SEESIB, UMR 6504, CNRS, F-63177 Aubiere, France
[2] SERVIER, Inst Rech, Div Rech Cancerol, F-78290 Croissy Sur Seine, France
关键词
isogranulatimide; antitumor agents; dipyrrolo[3,4-a : 3,4c]carbazole-1,3,4,6-tetraone; Chk1; inhibitors;
D O I
10.1016/j.bmc.2006.01.030
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The syntheses of a series of dipyrrolo[3,4-a:3,4-c]carbazole-1,3,4,6-tetraoties, substituted in 10-position with saturated and unsaturated side chains, via palladium catalyzed cross-coupling reactions, are described. These compounds call be considered as granulatimide bis-imide analogues. Their inhibitory activity toward Chk1 kinase and their antiproliferative activities in vitro in four tumor cell lines are reported. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3825 / 3834
页数:10
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