咪唑并(1,2-a)噻吩并(3,2-e)吡嗪作为IKK-β抑制剂的合成及其构效关系
Synthesis and structure-activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-beta inhibitors.
作者信息
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
机构信息
Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA.
出版信息
Bioorg Med Chem Lett. 2007 Aug 1;17(15):4284-9. doi: 10.1016/j.bmcl.2007.05.031. Epub 2007 May 16.
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.
描述了基于咪唑并噻吩并吡嗪模板鉴定出一系列有效的IKK-β选择性抑制剂，以及其中一种类似物（22j）在脂多糖诱导的肿瘤坏死因子-α释放小鼠模型中的口服疗效。
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