Department of Chemistry, University of Zürich, Winterthurerstrasse 190, CH-8057 Zürich, Switzerland.
Department of Biochemistry, University of Zürich, Winterthurerstrasse 190, CH-8057 Zürich, Switzerland.
Eur J Med Chem. 2016 Apr 13;112:347-366. doi: 10.1016/j.ejmech.2016.01.057. Epub 2016 Feb 2.
Several selective and potent EphB4 inhibitors have been discovered, optimized and biophysically characterized by our groups over the past years. On the outset of these discoveries high throughput docking techniques were applied. Herein, we review the optimization campaigns started from three of these hits (Xan-A1, Pyr-A1 and Qui-A1) with emphasis on their in depth in vitro and in vivo characterization, together with previously unpublished angiogenesis and fluorescence based assays.
在过去的几年中，我们小组发现、优化并通过生物物理特性对几种选择性和有效的 EphB4 抑制剂进行了研究。在这些发现的初始阶段，我们应用了高通量对接技术。在此，我们回顾了从这三种化合物（Xan-A1、Pyr-A1 和 Qui-A1）开始的优化研究，重点介绍了它们的深入的体外和体内特性，以及以前未发表的血管生成和荧光测定法。
