Cancer Research, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA.
Bioorg Med Chem Lett. 2009 Feb 1;19(3):1026-9. doi: 10.1016/j.bmcl.2008.10.053. Epub 2008 Oct 15.
A series of amidoheteroaryl compounds were designed and synthesized as inhibitors of B-Raf kinase. Several compounds from the series show excellent potency in biochemical, phenotypic and mode of action cellular assays. Potent examples from the series have also demonstrated good plasma exposure following an oral dose in rodents and activity against the Ras-Raf pathway in tumor bearing mice.
一系列酰胺杂芳基化合物被设计并合成出来，作为 B-Raf 激酶的抑制剂。该系列中的几种化合物在生化、表型和作用模式细胞测定中表现出优异的活性。该系列中的有效实例在啮齿动物口服给药后也显示出良好的血浆暴露，并对荷瘤小鼠中的 Ras-Raf 通路具有活性。
