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The azaindole framework in the design of kinase inhibitors.

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.

SUBMITTER: Merour JY

PROVIDER: S-EPMC6271083 | biostudies-literature | 2014 Nov

REPOSITORIES: biostudies-literature

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The azaindole framework in the design of kinase inhibitors.

Mérour Jean-Yves JY Buron Frédéric F Plé Karen K Bonnet Pascal P Routier Sylvain S

Molecules (Basel, Switzerland) 20141128 12

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 mod ...[more]

PMID: 25460315

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