Inhibitors of the tyrosine kinase EphB4. Part 2: Structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines
Inhibitors of the tyrosine kinase EphB4. Part 2: Structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines
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DOI：
10.1016/j.bmcl.2008.09.087
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发表时间：
2008-11-01
影响因子：
2.7
通讯作者：
Williams, Emma J.
中科院分区：
文献类型：
--
作者：
Bardelle, Catherine;Coleman, Tanya;Williams, Emma J.
对一系列EphB4的3 - 取代苯胺嘧啶抑制剂的晶体学研究突出了两种可供选择的C - 2苯胺构象，并且这一发现已被用于设计一系列高效的3,5 - 二取代苯胺嘧啶。所观察到的细胞活性范围已根据物理化学和结构特征得到合理的解释。(C) 2008爱思唯尔有限公司。保留所有权利。
Crystallographic studies of a range of 3-substituted anilinopyrimidine inhibitors of EphB4 have highlighted two alternative C-2 aniline conformations and this discovery has been exploited in the design of a highly potent series of 3,5-disubstituted anilinopyrimidines. The observed range of cellular activities has been rationalised on the basis of physicochemical and structural characteristics. (C) 2008 Elsevier Ltd. All rights reserved.