Inhibitors of the tyrosine kinase EphB4. Part 4: Discovery and optimization of a benzylic alcohol series
Inhibitors of the tyrosine kinase EphB4. Part 4: Discovery and optimization of a benzylic alcohol series
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DOI：
10.1016/j.bmcl.2011.03.009
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发表时间：
2011-04-15
影响因子：
2.7
通讯作者：
Read, Jon
中科院分区：
文献类型：
--
作者：
Barlaam, Bernard;Ducray, Richard;Read, Jon
我们的双苯胺基嘧啶系列 EphB4 激酶抑制剂的优化导致了化合物 12 的发现，该化合物在 C4 苯胺上结合了一个关键的间羟亚甲基。图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，表明它是研究EphB4激酶抑制剂的治疗潜力的合适候选者。 (C) 2011 Elsevier Ltd. 保留所有权利。
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. (C) 2011 Elsevier Ltd. All rights reserved.