861879-29-0Relevant academic research and scientific papers
Novel 2,3-dihydro-1,4-benzoxazines as potent and orally bioavailable inhibitors of tumor-driven angiogenesis
La, Daniel S.,Belzile, Julie,Bready, James V.,Coxon, Angela,DeMelfi, Thomas,Doerr, Nicholas,Estrada, Juan,Flynn, Julie C.,Flynn, Shaun R.,Graceffa, Russell F.,Harriman, Shawn P.,Larrow, Jay F.,Long, Alexander M.,Martin, Matthew W.,Morrison, Michael J.,Patel, Vinod F.,Roveto, Philip M.,Wang, Ling,Weiss, Matthew M.,Whittington, Douglas A.,Teffera, Yohannes,Zhao, Zhiyang,Polverino, Anthony J.,Harmange, Jean-Christophe
, p. 1695 - 1705 (2008/09/20)
Angiogenesis is vital for solid tumor growth, and its prevention is a proven strategy for the treatment of disease states such as cancer. The vascular endothelial growth factor (VEGF) pathway provides several opportunities by which small molecules can act as inhibitors of endothelial proliferation and migration. Critical to these processes is signaling through VEGFR-2 or the kinase insert domain receptor (KDR) upon stimulation by its ligand VEGF. Herein, we report the discovery of 2,3-dihydro-1,4-benzoxazines as inhibitors of intrinsic KDR activity (IC50 50 a potent (KDR: a promising platform for generating kinase-based antiangiogenic therapeutic agents.
