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

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

Affiliation

  • 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.

Figures
Products