219773-53-2Relevant academic research and scientific papers
Discovery of novel small molecule cell type-specific enhancers of NF-κB nuclear translocation
Gong, Gangli,Xie, Yuli,Liu, Yidong,Rinderspacher, Alison,Deng, Shi-Xian,Feng, Yan,Zhu, Zhengxiang,Tang, Yufei,Wyler, Michael,Aulner, Nathalie,Toebben, Udo,Smith, Deborah H.,Branden, Lars,Chung, Caty,Schuerer, Stephan,Vidovic, Dusica,Landry, Donald W.
scheme or table, p. 1191 - 1194 (2009/08/07)
An IKKβ inhibitor reported to block NF-κB transcriptional activities in Jurkat T cells, was found to enhance NF-κB translocation in HUVEC cells. These studies suggested a noncanonical NF-κB signaling pathway independent of IKKβ in HUVEC cells.
The design and synthesis of novel orally active inhibitors of AP-1 and NF-κB mediated transcriptional activation. SAR of in vitro and in vivo studies
Palanki, Moorthy S. S.,Erdman, Paul E.,Ren, Minghuan,Suto, Mark,Bennett, Brydon L.,Manning, Anthony,Ransone, Lynn,Spooner, Cheryl,Desai, Sonal,Ow, Arnie,Totsuka, Ryuichi,Tsao, Peter,Toriumi, Wataru
, p. 4077 - 4080 (2007/10/03)
We have developed novel orally active quinazoline analogues as inhibitors of AP-1 and NF-κB mediated transcriptional activation. Among the derivatives prepared, 1-[2-(2-thienyl)quinazolin-4-ylamino]-3-methyl-3- pyrroline-2,5-dione (10) showed significant activity in an adjuvant-induced arthritis rat model by reducing the swelling by 65% in the non-injected foot. The synthesis, structure-activity relationship, and in vivo activity are described.
