运用生物等排原理发现强效 Aurora 激酶抑制剂咪唑并[1,2-a]吡嗪。
Bioisosteric approach to the discovery of imidazo[1,2-a]pyrazines as potent Aurora kinase inhibitors.
机构信息
Department of Chemistry, Merck Research Laboratories, 320 Bent Street, Cambridge, MA 02141, United States.
出版信息
Bioorg Med Chem Lett. 2011 Jan 1;21(1):592-8. doi: 10.1016/j.bmcl.2010.10.008. Epub 2010 Oct 12.
PMID:21075632
Abstract
Our continued effort toward the development of the imidazo[1,2-a]pyrazine scaffold as Aurora kinase inhibitors is described. Bioisosteric approach was applied to optimize the 8-position of the core. Several new potent Aurora A/B dual inhibitors, such as 25k and 25l, were identified.
摘要
我们一直在努力开发咪唑并[1,2-a]吡嗪骨架作为 Aurora 激酶抑制剂。本文应用生物等排体方法对核心的 8 位进行了优化。鉴定出了几种新的有效的 Aurora A/B 双重抑制剂，如 25k 和 25l。
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