Next Article in Journal
Anti-Proliferative Effects of Siegesbeckia orientalis Ethanol Extract on Human Endometrial RL-95 Cancer Cells
Next Article in Special Issue
Stability of the Human Hsp90-p50Cdc37 Chaperone Complex against Nucleotides and Hsp90 Inhibitors, and the Influence of Phosphorylation by Casein Kinase 2
Previous Article in Journal
Antibacterial and EGFR-Tyrosine Kinase Inhibitory Activities of Polyhydroxylated Xanthones from Garcinia succifolia
Previous Article in Special Issue
Therapeutic Targeting the Cell Division Cycle 25 (CDC25) Phosphatases in Human Acute Myeloid Leukemia — The Possibility to Target Several Kinases through Inhibition of the Various CDC25 Isoforms
Open AccessReview

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.
Molecules 2014, 19(12), 19935-19979; https://doi.org/10.3390/molecules191219935
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
Show Figures

Graphical abstract

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.

Show more citation formats Show less citations formats

Article Access Map by Country/Region

1
Only visits after 24 November 2015 are recorded.
Back to TopTop