发现苯并恶唑取代的氨基吡啶作为口服活性的 c-Met 激酶抑制剂。
Discovery of aminopyridines substituted with benzoxazole as orally active c-Met kinase inhibitors.
机构信息
Bio-Organic Science Division, Korea Research Institute of Chemical Technology, PO Box 107, Daejeon 305-600, Republic of Korea.
出版信息
Bioorg Med Chem Lett. 2010 Jul 15;20(14):4223-7. doi: 10.1016/j.bmcl.2010.05.031. Epub 2010 May 15.
PMID:20570511
Abstract
We report the synthesis and biological evaluation of aminopyridines substituted with benzoxazole. The SAR of the aminopyridines was explored to improve the inhibitory activity against c-Met and to decrease hERG affinity. These studies led to the discovery of amide 24 which showed good c-Met inhibitory potency, low affinity to hERG and favorable pharmacokinetic properties in rats.
摘要
我们报告了苯并恶唑取代的氨基吡啶的合成和生物学评价。我们对氨基吡啶进行了 SAR 研究，以提高对 c-Met 的抑制活性并降低 hERG 亲和力。这些研究导致酰胺 24 的发现，其显示出良好的 c-Met 抑制效力、对 hERG 的低亲和力和在大鼠中良好的药代动力学性质。
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