开发含有芳基磺酰胺头基的强效 B-RafV600E 抑制剂。
Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.
机构信息
GlaxoSmithKline Oncology CEDD, Research Triangle Park, NC 27709-3398, United States.
出版信息
Bioorg Med Chem Lett. 2011 Aug 1;21(15):4436-40. doi: 10.1016/j.bmcl.2011.06.021. Epub 2011 Jun 16.
PMID:21733693
Abstract
A potent series of inhibitors against the B-Raf(V600E) kinase have been developed that show excellent activity in cellular assays and good oral bioavailability in rats. The key structural features of the series are an arylsulfonamide headgroup, a thiazole core, and a fluorine ortho to the sulfonamide nitrogen.
摘要
已经开发出了一系列强效的 B-Raf(V600E)激酶抑制剂，它们在细胞测定中显示出优异的活性，并且在大鼠中具有良好的口服生物利用度。该系列的关键结构特征是芳基磺酰胺头基、噻唑核心以及磺酰胺氮的邻位氟原子。
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