Discovery and optimization of pyrazoline compounds as B-Raf inhibitors

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• 作者：Matthew O. Duffey ; Ruth Adams ; Christopher Blackburn ; Ryan W. Chau ; Susan Chen ; Katherine M. Galvin ; Khristofer Garcia ; Alex ; ra E. Gould ; Paul D. Greenspan ; Sean Harrison ; Shih-Chung Huang ; Mi-Sook Ki
• 关键词：B-Raf ; B-Raf inhibitor ; Pyrazoline
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：15 August 2010
• 年：2010
• 卷：20
• 期：16
• 页码：4800-4804
• 全文大小：1868 K

文摘

The discovery of novel pyrazoline derivatives as B-Raf (V600E) inhibitors is described in this report. Chemical modification of the pyrazoline scaffold led to the development of SAR and identified potent and selective inhibitors of B-Raf (V600E). Determination of the pharmacokinetic properties of selected inhibitors is also reported.