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

  • Bioorg Med Chem Lett. 2007 Aug 1;17(15):4284-9. doi: 10.1016/j.bmcl.2007.05.031.
Makonen Belema  1 ,  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
Affiliations
  • 1. Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. [email protected]
PMID: 17540562 DOI: 10.1016/j.bmcl.2007.05.031
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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