Download MendeleyPyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase.
Cee, V.J., Cheng, A.C., Romero, K., Bellon, S., Mohr, C., Whittington, D.A., Bak, A., Bready, J., Caenepeel, S., Coxon, A., Deak, H.L., Fretland, J., Gu, Y., Hodous, B.L., Huang, X., Kim, J.L., Lin, J., Long, A.M., Nguyen, H., Olivieri, P.R., Patel, V.F., Wang, L., Zhou, Y., Hughes, P., Geuns-Meyer, S.(2009) Bioorg Med Chem Lett 19: 424-427
- PubMed: 19062275
- DOI: https://doi.org/10.1016/j.bmcl.2008.11.056
- Primary Citation of Related Structures:
3DA6, 3EFW, 3EWH - PubMed Abstract:
Selective small molecule inhibitors of Tie-2 kinase are important tools for the validation of Tie-2 signaling in pathological angiogenesis. Reported herein is the optimization of a nonselective scaffold into a potent and highly selective inhibitor of Tie-2 kinase.
Organizational Affiliation:
Department of Medicinal Chemistry, Amgen Inc., One Kendall Square, Bldg. 1000, Cambridge, MA 02139, USA. vcee@amgen.com
