Structure activity relationship of selected polyphenol derivatives as inhibitors of Bax/Bcl-xL interaction

被引：14

作者：

Vo, Duc Duy ^{[1
]}

Gautier, Fabien ^{[2
,3
]}

Juin, Philippe ^{[2
]}

Gree, Rene ^{[1
]}

机构：

[1] Univ Rennes 1, Lab Sci Chim Rennes, CNRS UMR 6226, F-35042 Rennes, France

[2] Univ Nantes, CRCNA INSERM U892, F-44007 Nantes 1, France

[3] Ctr Rech Cancerol, Inst Cancerol Ouest, Nantes, France

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 51卷

关键词：

Phenol; Bax; Bcl-xL; Apoptosis; BRET; Cancer; BCL-2; FAMILY-MEMBERS; SMALL-MOLECULE INHIBITORS; PROGRAMMED CELL-DEATH; BH3 MIMETIC ABT-737; CANCER; APOPTOSIS; TARGETS; MCL-1; SENSITIVITY; MECHANISMS;

D O I：

10.1016/j.ejmech.2012.02.036

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This paper describes the synthesis of nine selected diaryl/heteroaryl-containing phenol and polyphenol derivatives which have been evaluated against Bax/Bcl-xL interaction in comparison with ABT-737. Using a BRET assay, six of these derivatives exhibit activity comparable to ABT-737 to disrupt Bax/Bcl-xL interaction. These preliminary results demonstrate that such polyphenol-derived molecules are attractive compounds regarding anticancer activity and that the phenol at position 3 is important regarding disruption of Bax/Bcl-xL interaction. (C) 2012 Elsevier Masson SAS. All rights reserved.

引用

页码：286 / 293

页数：8

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