Discovery of protein-protein binding disruptors using multi-component condensations small molecules

被引：56

作者：

Bedjeguelal, Karim ^{[1
]}

Bienayme, Hugues ^{[1
]}

Dumoulin, Antoine ^{[1
]}

Poigny, Stephane ^{[1
]}

Schmitt, Philippe ^{[1
]}

Tam, Eric ^{[1
]}

机构：

[1] Pierre Fabre Urol, F-69100 Villeurbanne, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 15期

关键词：

VEGF-NRP1; protein-protein interaction; multi-component condensations; 3-amino-1-cyano-indolizines;

D O I：

10.1016/j.bmcl.2006.05.014

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of small molecule compounds interfering with the binding process of VEGF and NRP1 has been identified and further optimized. Full synthetic details as well as SAR are reported which demonstrate that expeditious MCC-based syntheses may lead to valuable molecules addressing challenging targets such as protein-protein interactions. Preliminary functional assay data confirm that these compounds may be further developed toward drug candidates. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：3998 / 4001

页数：4

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