Synthesis and structure–activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-β inhibitors

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• 作者：Makonen Belema ; Amy Bunker ; Van N. Nguyen ; Francis Beaulieu ; Carl Ouellet ; Yuping Qiu ; Yunhui Zhang ; Alain Martel ; James R. Burke ; Kim W. McIntyre ; Mark A. Pattoli ; Connie Daloisio ; Kathleen M. Gilloo
• 关键词：IKK ; NF-κ ; B ; TNF-α ; Imidazothienopyrazine
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 出版时间：1 August 2007
• 年：2007
• 卷：17
• 期：15
• 页码：4284-4289
• 全文大小：172 K

文摘

The identification of a potent series of IKK-β selective inhibitors based on an imidazothienopyrazine template and the oral efficacy of one such analog (22j) in the LPS-induced TNF-α release mouse model are described.