发现咪唑并[1,2-a]吡嗪类 Aurora 激酶抑制剂。
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
机构信息
Department of Chemistry, Merck Research Laboratories, Cambridge, MA 02141, USA.
出版信息
Bioorg Med Chem Lett. 2010 Sep 1;20(17):5170-4. doi: 10.1016/j.bmcl.2010.07.008. Epub 2010 Jul 8.
PMID:20674350
Abstract
The synthesis and structure-activity relationships (SAR) of novel, potent imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors are described. The X-ray crystal structure of imidazo[1,2-a]pyrazine Aurora inhibitor 1j is disclosed. Compound 10i was identified as lead compound with a promising overall profile.
摘要
本文描述了新型强效咪唑并[1,2-a]吡嗪类 Aurora 激酶抑制剂的合成及构效关系（SAR）。公开了咪唑并[1,2-a]吡嗪 Aurora 抑制剂 1j 的 X 射线晶体结构。化合物 10i 被确定为具有良好综合特性的先导化合物。
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