Imidazopyridine-fused [1,3] -diazepinones: Synthesis and antiproliferative activity

被引：45

作者：

Gallud, Audrey ^{[1
,2
]}

Vaillant, Ophelie ^{[1
,2
]}

Maillard, Ludovic T. ^{[1
,2
]}

Arama, Dominique P. ^{[1
,2
]}

Dubois, Joelle ^{[3
]}

Maynadier, Marie ^{[1
,2
]}

Lisowski, Vincent ^{[1
,2
]}

Garcia, Marcel ^{[1
,2
]}

Martinez, Jean ^{[1
,2
]}

Masurier, Nicolas ^{[1
,2
]}

机构：

[1] Univ Montpellier I, CNRS, UMR 5247, Inst Biomol Max Mousseron, F-34093 Montpellier 5, France

[2] Univ Montpellier 2, UFR Sci Pharmaceut & Biol, F-34093 Montpellier 5, France

[3] CNRS, Ctr Rech Gif, UPR 2301, Inst Chim Subst Nat, F-91198 Gif Sur Yvette, France

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 75卷

关键词：

Imidazo[1,2-a]pyridine; Polyfused heterocycles; Diazepinones; Antitumor activity; HGK inhibitors; GLYCOGEN-SYNTHASE KINASE-3-BETA; DEPENDENT KINASE INHIBITOR; ERM PROTEINS; PAULLONES; SCREEN; CANCER; HGK; EXPRESSION; DISCOVERY; INVASION;

D O I：

10.1016/j.ejmech.2014.01.044

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 15 pyrido-imidazo-1,3-diazepin-5-ones and pyrido-1,3-diazepine-2,5-diones were synthesized and their anticancer activities were evaluated. Among tested compounds on a cell lines panel, compound 6a presents the best growth inhibition activity on 21 cell lines with a cytotoxic effect on MDA-MB-435 melanoma cells. This compound led to deep cell morphological changes and revealed to be an inhibitor of the Hepatocyte progenitor kinase-like kinase (HGK), which is known to be implicated in the migration, adhesion and invasion of various tumor cells. (C) 2014 Elsevier Masson SAS. All rights reserved.

引用

页码：382 / 390

页数：9

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