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.

The results of research into the chemistry of 7-azaindole during the last twenty years are presented. New synthetic methods for the 7-azaindole structures are developed including palladium-catalysed cross-coupling reactions. Reactivity of 3-formyl-, 3-halogeno- and 2-lithio-7-azaindole derivatives is reported. Functionalisation of the pyridine ring via the N-oxide is also described. In the last part, biological activity of various 7-azaindole derivatives is briefly indicated.

Functionalisation at C-2 and C-3 of N-protected-5-azaindole leads to a variety of very useful new substituted 5-azaindole derivatives in fair to good yields.