Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity
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- 作者：Paul D. Lyne ; Brian Aquila ; Donald J. Cook ; Les A. Dakin ; Jay Ezhuthachan ; Stephanos Ioannidis ; Timothy Pontz ; Mei Su ; Qing Ye ; Xiaolan Zheng ; Michael H. Block ; Scott Cowen ; Tracy L. Deegan ; John W. L
- 关键词：B-Raf ; V600E ; Amidoheteroaryl
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2009
- 出版时间：1 February 2009
- 年：2009
- 卷：19
- 期：3
- 页码：1026-1029
- 全文大小：218 K
文摘
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.