Mérour Jean-Yves, Buron Frédéric, Plé Karen, Bonnet Pascal, Routier Sylvain
Institut de Chimie Organique et Analytique (ICOA), Université d'Orléans, UMR CNRS 7311, Orléans F-45067, France.
Molecules. 2014 Nov 28;19(12):19935-79. doi: 10.3390/molecules191219935.
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.
这篇综述文章阐述了氮杂吲哚衍生物作为激酶抑制剂的使用日益增加,以及它们对药物发现和创新的贡献。文中介绍了作为靶点的不同蛋白激酶,以及从药物化学和基于片段的药物发现(FBDD)项目中产生的已知分子。还讨论了用于制备这些化合物的各种合成路线以及导致其合成的化学途径。基于X射线晶体学数据对它们的结合模式进行分析,为设计更有效和更具选择性的抑制剂提供了结构方面的见解。