The Discovery of furo[2,3-c]pyridine-based indanone oximes as potent and selective B-Raf inhibitors

被引：25

作者：

Buckmelter, Alex J. ^{[1
]}

Ren, Li ^{[1
]}

Laird, Ellen R. ^{[1
]}

Rast, Bryson ^{[1
]}

Miknis, Greg ^{[1
]}

Wenglowsky, Steve ^{[1
]}

Schlachter, Stephen ^{[1
]}

Welch, Mike ^{[1
]}

Tarlton, Eugene ^{[1
]}

Grina, Jonas ^{[1
]}

Lyssikatos, Joseph ^{[2
]}

Brandhuber, Barbara J. ^{[1
]}

Morales, Tony ^{[1
]}

Randolph, Nikole ^{[1
]}

Vigers, Guy ^{[1
]}

Martinson, Matthew ^{[1
]}

Callejo, Michele ^{[1
]}

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 / 04期

关键词：

B-Raf; Kinase; Cancer therapy; DESIGN; KINASE; MUTATIONS; PYRAZINES; ENERGY;

D O I：

10.1016/j.bmcl.2010.12.039

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Virtual and high-throughput screening identified imidazo[1,2-a]pyrazines as inhibitors of B-Raf. We describe the rationale, SAR, and evolution of the initial hits to a series of furo[2,3-c]pyridine indanone oximes as highly potent and selective inhibitors of B-Raf. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：1248 / 1252

页数：5

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