Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors

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• 作者：Sharadha Subramanian ; Abran Costales ; Teresa E. Williams ; Barry Levine ; Christopher M. McBride ; Daniel Poon ; Payman Amiri ; Paul A. Renhowe ; Cynthia M. Shafer ; Darrin Stuart ; Joelle Verhagen ; Savithri Ramurthy
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2014
• 出版时间：September 11, 2014
• 年：2014
• 卷：5
• 期：9
• 页码：989-992
• 全文大小：240K
• ISSN：1948-5875

文摘

Benzimidazole reverse amides were designed and synthesized as Pan RAF kinase inhibitors. Investigation of the structure鈥揳ctivity relationship of the compounds revealed that they were potent in vitro and exhibited desirable in vivo properties.

Keywords:

MAP; ras-mitogen activated protein kinase; VEGF; vascular endothelial growth factor receptor; CSF1R; colony stimulating factor-1 receptor; RTKs; receptor tyrosine kinases; STKs; serine threonine kinases; TKs; tyrosine kinases