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Synthesis and structure-activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-beta inhibitors |
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| 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 |
| Affiliation: | Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. makonen.belema@bms.com |
| Abstract: | The identification of a potent series of IKK-beta selective inhibitors based on an imidazothienopyrazine template and the oral efficacy of one such analog (22j) in the LPS-induced TNF-alpha release mouse model are described. |
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