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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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| Published in: | Bioorganic & medicinal chemistry letters 2007-08, Vol.17 (15), p.4284-4289 |
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| Main Authors: | , , , , , , , , , , , , , , , , |
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| Language: | English |
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| cites | cdi_FETCH-LOGICAL-c415t-64209165248acf410925983b58e68abbb81ebec45ff161c3e2951fe5629c0c43 |
| container_end_page | 4289 |
| container_issue | 15 |
| container_start_page | 4284 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 17 |
| creator | 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. |
| description | 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. |
| doi_str_mv | 10.1016/j.bmcl.2007.05.031 |
| format | article |
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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.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Bones, joints and connective tissue. Antiinflammatory agents</subject><subject>Cells, Cultured</subject><subject>Enzyme Inhibitors - chemical synthesis</subject><subject>Enzyme Inhibitors - chemistry</subject><subject>Enzyme Inhibitors - pharmacology</subject><subject>Humans</subject><subject>I-kappa B Kinase - antagonists & inhibitors</subject><subject>IKK</subject><subject>Imidazothienopyrazine</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>NF-κB</subject><subject>Pharmacology. 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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.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>17540562</pmid><doi>10.1016/j.bmcl.2007.05.031</doi><tpages>6</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2007-08, Vol.17 (15), p.4284-4289 |
| issn | 0960-894X 1464-3405 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_70699993 |
| source | ScienceDirect Freedom Collection |
| 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 |
| title | Synthesis and structure–activity relationship of imidazo(1,2- a)thieno(3,2- e)pyrazines as IKK-β inhibitors |
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