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Molecules 2014, 19(12), 19935-19979;

The Azaindole Framework in the Design of Kinase Inhibitors

Institut de Chimie Organique et Analytique (ICOA), Université d'Orléans, UMR CNRS 7311, Orléans F-45067, France
Author to whom correspondence should be addressed.
Received: 16 October 2014 / Revised: 10 November 2014 / Accepted: 18 November 2014 / Published: 28 November 2014
(This article belongs to the Special Issue Design and Study of Kinase Inhibitors)


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. View Full-Text
Keywords: azaindoles; kinase inhibitors; kinase binding mode; structural analysis azaindoles; kinase inhibitors; kinase binding mode; structural analysis

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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MDPI and ACS Style

Mérour, J.-Y.; Buron, F.; Plé, K.; Bonnet, P.; Routier, S. The Azaindole Framework in the Design of Kinase Inhibitors. Molecules 2014, 19, 19935-19979.

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