The Azaindole Framework in the Design of Kinase Inhibitors

Molecules

Jean-Yves Mérour²  Frຝéric Buron²  Karen Plé²  Pascal Bonnet²  Sylvain Routier¹ 

[1] Institut de Chimie Organique et Analytique (ICOA), Université d’Orléans, UMR CNRS 7311, Orléans F-45067, France;

关键词: azaindoles;    kinase inhibitors;    kinase binding mode;    structural analysis;   

DOI  :  10.3390/molecules191219935

来源: mdpi

【 摘 要 】

This review article illustrates the growing use of azaindole derivatives as kinase inhibitors and their contribution to drug discovery and innovation. The different protein kinases which have served as targets and the known molecules which have emerged from medicinal chemistry and Fragment-Based Drug Discovery (FBDD) programs are presented. The various synthetic routes used to access these compounds and the chemical pathways leading to their synthesis are also discussed. An analysis of their mode of binding based on X-ray crystallography data gives structural insights for the design of more potent and selective inhibitors.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.