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

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. The identification of a potent series of IKK-β selective inhibitors based on an i...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2007-08, Vol.17 (15), p.4284-4289
Main Authors: Belema, Makonen, Bunker, Amy, Nguyen, Van N., Beaulieu, Francis, Ouellet, Carl, Qiu, Yuping, Zhang, Yunhui, Martel, Alain, Burke, James R., McIntyre, Kim W., Pattoli, Mark A., Daloisio, Connie, Gillooly, Kathleen M., Clarke, Wendy J., Brassil, Patrick J., Zusi, F. Chris, Vyas, Dolatrai M.
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Cells, Cultured
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Humans
I-kappa B Kinase - antagonists & inhibitors
IKK
Imidazothienopyrazine
Medical sciences
Mice
NF-κB
Pharmacology. Drug treatments
Pyrazines - chemical synthesis
Pyrazines - chemistry
Pyrazines - pharmacology
Structure-Activity Relationship
TNF-α
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Summary: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. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.05.031