AstraZeneca, Centre de Recherches, Z.I. la Pompelle, BP1050, 51689 Reims, Cedex 2, France.
Bioorg Med Chem Lett. 2011 Apr 15;21(8):2207-11. doi: 10.1016/j.bmcl.2011.03.009.
Optimization of our bis-anilino-pyrimidine series of EphB4 kinase inhibitors led to the discovery of compound 12 which incorporates a key m-hydroxymethylene group on the C4 aniline. 12 displays a good kinase selectivity profile, good physical properties and pharmacokinetic parameters, suggesting it is a suitable candidate to investigate the therapeutic potential of EphB4 kinase inhibitors.
我们对双苯胺嘧啶系列 EphB4 激酶抑制剂进行了优化，发现了化合物 12，其中在 C4 苯胺上引入了关键的 m-羟基亚甲基。12 显示出良好的激酶选择性特征、良好的物理性质和药代动力学参数，表明它是一个合适的候选物，可以研究 EphB4 激酶抑制剂的治疗潜力。
