2-氨基芳基-7-芳基苯并恶唑作为有效、选择性和口服有效的 JAK2 抑制剂。
2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.
机构信息
Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4002 Basel, Switzerland.
出版信息
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1724-7. doi: 10.1016/j.bmcl.2010.01.069. Epub 2010 Jan 21.
PMID:20138510
Abstract
A series of novel benzoxazole derivatives has been designed and shown to exhibit attractive JAK2 inhibitory profiles in biochemical and cellular assays, capable of delivering compounds with favorable PK properties in rats. Synthesis and structure-activity relationship data are also provided.
摘要
一系列新型苯并恶唑衍生物被设计并在生化和细胞测定中显示出有吸引力的 JAK2 抑制特性，能够在大鼠中提供具有良好 PK 性质的化合物。还提供了合成和构效关系数据。
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