501684-31-7Relevant academic research and scientific papers
Inhibition of Tpl2 kinase and TNFα production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis
Hu, Yonghan,Green, Neal,Gavrin, Lori K.,Janz, Kristin,Kaila, Neelu,Li, Huan-Qiu,Thomason, Jennifer R.,Cuozzo, John W.,Hall, J. Perry,Hsu, Sang,Nickerson-Nutter, Cheryl,Telliez, Jean-Baptiste,Lin, Lih-Ling,Tam, Steve
, p. 6067 - 6072 (2007/10/03)
The synthesis and structure-activity studies of a series of quinoline-3-carbonitriles as inhibitors of Tpl2 kinase are described. Potent inhibitors of Tpl2 kinase with selectivity against a panel of selected kinases in enzymatic assays and specificity in cell-based phosphorylation assays in LPS-treated human monocytes were identified. Selected inhibitors with moderate activity in human whole blood assay effectively inhibited LPS/D-Gal induced TNFα release when administered intraperitoneally in mice.
Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: Analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents
Wissner, Allan,Brawner Floyd,Rabindran, Sridhar K.,Nilakantan, Ramaswamy,Greenberger, Lee M.,Shen, Ru,Wang, Yu-Fen,Tsou, Hwei-Ru
, p. 2893 - 2897 (2007/10/03)
The syntheses and biological evaluations of 4-anilinoquinoline-3-carbonitrile analogues of the three clinical lead 4-anilinoquinazolines Iressa, Tarceva, and CI-1033 are described. The EGFR and HER-2 kinase inhibitory activities and the cell growth inhibition of the two series are compared with each other and with the clinical lead EKB-569. Similar activities are observed between these two series.
