Synthesis and biological activities of aminopyrimidyl-indoles structurally related to meridianins

被引：69

作者：

Akue-Gedu, Rufine ^{[1
,2
]}

Debiton, Eric ^{[3
]}

Ferandin, Yoan ^{[4
]}

Meijer, Laurent ^{[4
]}

Prudhomme, Michelle ^{[1
,2
]}

Anizon, Fabrice ^{[1
,2
]}

Moreau, Pascale ^{[1
,2
]}

机构：

[1] Univ Clermont Ferrand, Clermont Univ, SEESIB, F-63177 Aubiere, France

[2] CNRS, UMR 6504, F-63177 Aubiere, France

[3] Univ Auvergne, Clermont Univ, Ctr Jean Perrin, F-63005 Clermont Ferrand, France

[4] CNRS, Biol Stn, Prot Phosphorylat & Human Dis Grp, F-29682 Roscoff, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 13期

关键词：

Meridianins; Suzuki cross-coupling; Kinase inhibitors; Dyrk1A inhibitors; SYNDROME CRITICAL REGION; KINASE INHIBITORS; AFFINITY-CHROMATOGRAPHY; APLIDIUM-MERIDIANUM; TAU-PHOSPHORYLATION; IMMOBILIZED AXIN; PROTEIN-KINASES; PURIFICATION; MERIOLINS; DISEASE;

D O I：

10.1016/j.bmc.2009.05.017

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 synthesis of new meridianin derivatives substituted at the C-5 position of the 2-aminopyrimidine ring by various aryl groups and substituted or not by a methyl group on the indole nitrogen is described. These compounds were tested for their kinase inhibitory potencies toward five kinases (CDK5/p25, CK1 delta/epsilon, GSK-3 alpha/beta, Dyrk1A and Erk2) as well as their in vitro antiproliferative activities toward a human fibroblast primary culture and two human solid cancer cell lines (MCF-7 and PA 1). (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：4420 / 4424

页数：5

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