An amino-indazole scaffold with spectrum selective kinase inhibition of FLT3, PDGFR¦Á and kit

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• 作者：Xianming Deng ; Wenjun Zhou ; Ellen Weisberg ; Jinhua Wang ; Jianming Zhang ; Takaaki Sasaki ; Erik Nelson ; James D. Griffin ; Pasi A. J?nne ; Nathanael S. Gray
• 关键词：FVESJAXAINWQOW-UHFFFAOYSA-N ; ASNRYHMAHRHWQB-UHFFFAOYSA-N
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 出版时间：15 July, 2012
• 年：2012
• 卷：22
• 期：14
• 页码：4579-4584
• 全文大小：2056 K

文摘

Here we describe the synthesis and characterization of a number of 3-amino-1H-indazol-6-yl-benzamides that were designed to target the ¡®DFG-out¡¯ conformation of the kinase activation loop. Several compounds such as 4 and 11 exhibit single-digit nanomolar EC₅₀s against FLT3, c-Kit and the gatekeeper T674M mutant of PDGFR¦Á.