The Azaindole Framework in the Design of Kinase Inhibitors

Author: Mérour Jean-Yves   Buron Frédéric   Plé Karen   Bonnet Pascal   Routier Sylvain  

Publisher: MDPI

E-ISSN: 1420-3049|19|12|19935-19979

ISSN: 1420-3049

Source: Molecules, Vol.19, Iss.12, 2014-11, pp. : 19935-19979

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Abstract

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.