期刊
MOLECULES
卷 19, 期 12, 页码 19935-19979出版社
MDPI
DOI: 10.3390/molecules191219935
关键词
azaindoles; kinase inhibitors; kinase binding mode; structural analysis
资金
- INCa (National Cancer Institute)
- Ligue Contre le Cancer Inter-region du Grand Ouest
- Canceropole Grand Ouest CGO
- Valorisation des produits de la mer
- ARC Foundation for Cancer research
- Labex IRON [ANR-11-LABX-0018-01]
- Region Centre/FEDER (Cosmi programs)
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.
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