Ghada F. Elmasry

Design of 4-(piperazin-1-yl)thieno[2,3-d]pyrimidine derivatives targeting the DFG-out conformation of VEGFR-2: Synthesis, biological evaluations, and molecular modeling approaches.

Novel series of piperazinyl-thienopyrimidine acetamide derivatives (10a-l, 13a-b, and 16a) were rationally designed and synthesized as potential type II VEGFR-2 inhibitors based on the essential pharmacophoric features of sorafenib and the co-crystallized ligand in the VEGFR-2 crystal structure (PDB: 2OH4). The target...