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通过钯催化交叉偶联反应合成并带有各种饱和及不饱和侧链取代的新型二吡咯并[3,4-a:3,4-c]咔唑-1,3,4,6-四酮的生物学评价

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.

作者信息

Hénon Hélène, Anizon Fabrice, Golsteyn Roy M, Léonce Stéphane, Hofmann Robert, Pfeiffer Bruno, Prudhomme Michelle

机构信息

Laboratoire SEESIB, Université Blaise Pascal, UMR 6504 du CNRS, 63177 Aubière, France.

出版信息

Bioorg Med Chem. 2006 Jun 1;14(11):3825-34. doi: 10.1016/j.bmc.2006.01.030. Epub 2006 Feb 3.

Abstract

The syntheses of a series of dipyrrolo[3,4-a:3,4-c]carbazole-1,3,4,6-tetraones, substituted in 10-position with saturated and unsaturated side chains, via palladium catalyzed cross-coupling reactions, are described. These compounds can 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.

摘要

描述了一系列在10位被饱和和不饱和侧链取代的二吡咯并[3,4-a:3,4-c]咔唑-1,3,4,6-四酮通过钯催化交叉偶联反应的合成方法。这些化合物可被视为颗粒酰亚胺双酰亚胺类似物。报道了它们对Chk1激酶的抑制活性及其在四种肿瘤细胞系中的体外抗增殖活性。

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