Non-oxime pyrazole based inhibitors of B-Raf kinase

被引：42

作者：

Newhouse, Bradley J. ^{[1
]}

Hansen, Joshua D. ^{[1
]}

Grina, Jonas ^{[1
]}

Welch, Mike ^{[1
]}

Topalov, George ^{[1
]}

Littman, Nicole ^{[1
]}

Callejo, Michele ^{[1
]}

Martinson, Matthew ^{[1
]}

Galbraith, Sarah ^{[1
]}

Laird, Ellen R. ^{[1
]}

Brandhuber, Barbara J. ^{[1
]}

Vigers, Guy ^{[1
]}

Morales, Tony ^{[1
]}

Woessner, Rich ^{[1
]}

Randolph, Nikole ^{[1
]}

Lyssikatos, Joseph ^{[2
]}

Olivero, Alan ^{[2
]}

机构：

[1] Array BioPharma, Boulder, CO 80301 USA

[2] Genentech Inc, San Francisco, CA 94080 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 11期

关键词：

B-Raf; Oxime; Pyrazole; MEDICINAL CHEMISTRY; SIGNALING PATHWAY; BRAF GENE; ACTIVATION; MUTATIONS; FLUORINE; CANCER; OXYGEN;

D O I：

10.1016/j.bmcl.2010.12.038

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

The synthesis and biological evaluation of non-oxime pyrazole based B-Raf inhibitors is reported. Several oxime replacements have been prepared and have shown excellent enzyme activity. Further optimization of fused pyrazole 2a led to compound 38, a selective and potent B-Raf inhibitor. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：3488 / 3492

页数：5

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