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Pyr-A1 and Qui-A1) with emphasis on their in depth in vitro and in vivo characterization, together with previously unpublished angiogenesis and fluorescence based assays.
BT - European Journal of Medicinal Chemistry C1 - 0208 DA - 2016 Apr 13 DO - 10.1016/j.ejmech.2016.01.057 J2 - Eur. J. Med. Chem. LA - eng M3 - Review Article N2 -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Pyr-A1 and Qui-A1) with emphasis on their in depth in vitro and in vivo characterization, together with previously unpublished angiogenesis and fluorescence based assays.
PY - 2016 SE - 347 SP - 347 EP - 366 T2 - European Journal of Medicinal Chemistry TI - Three stories on Eph kinase inhibitors: From in silico discovery to in vivo validation VL - 112 SN - 1768-3254 ER -