Cee Victor J, Cheng Alan C, Romero Karina, Bellon Steve, Mohr Christopher, Whittington Douglas A, Bak Annette, Bready James, Caenepeel Sean, Coxon Angela, Deak Holly L, Fretland Jenne, Gu Yan, Hodous Brian L, Huang Xin, Kim Joseph L, Lin Jasmine, Long Alexander M, Nguyen Hanh, Olivieri Philip R, Patel Vinod F, Wang Ling, Zhou Yihong, Hughes Paul, Geuns-Meyer Stephanie
Department of Medicinal Chemistry, Amgen Inc., One Kendall Square, Bldg. 1000, Cambridge, MA 02139, USA.
Bioorg Med Chem Lett. 2009 Jan 15;19(2):424-7. doi: 10.1016/j.bmcl.2008.11.056. Epub 2008 Nov 20.
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.
Tie-2激酶的选择性小分子抑制剂是验证病理性血管生成中Tie-2信号传导的重要工具。本文报道了将一种非选择性骨架优化为Tie-2激酶的强效且高度选择性抑制剂的过程。
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