Synthesis of Thienopyrimidine Derivatives as Inhibitors of STAT3.
A series of thienopyrimidine compounds (6Aa-g and 6Ba-d) were synthesized and characterized by NMR spectroscopy and mass spectrometry. These compounds (6Aa-g and 6Ba-d) potently inhibited STAT3 expression induced by IL-6 in a dose-dependent manner with IC50 values of 5.73-0.32 μM. Among the prepared thienopyrimidine derivatives, 6Aa, 6Ab, 6Ba and 6Bc significantly suppressed the phosphorylation of STAT3 and ERK1/2 stimulated by IL-6 in Hep3B cells. Furthermore, the synthesized compounds might be useful remedies for the treatment of inflammatory diseases by inhibiting the action of IL-6.
['Jang|Hyun-Jae|HJ|', 'Kim|Sung Min|SM|', 'Rho|Mun-Chual|MC|', 'Lee|Seung Woong|SW|', 'Song|Yang-Heon|YH|']
D000893:Anti-Inflammatory Agents D045744:Cell Line, Tumor D002470:Cell Survival D004791:Enzyme Inhibitors D048049:Extracellular Signal-Regulated MAP Kinases D006801:Humans D015850:Interleukin-6 D015394:Molecular Structure D010766:Phosphorylation D011401:Promoter Regions, Genetic D011743:Pyrimidines D050796:STAT3 Transcription Factor
Thienopyrimidine derivatives STAT3 Interleukin-6 anti-inflammatory