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

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. Gillooly,Wendy J. Clarke,Patrick J. Brassil,F. Chris Zusi,Dolatrai M. Vyas

Bioorganic & Medicinal Chemistry Letters（2007）

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摘要

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.

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关键词

IKK,NF-κB,TNF-α,Imidazothienopyrazine

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