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KMID : 0545120190290060856
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Journal of Microbiology and Biotechnology
2019 Volume.29 No. 6 p.856 ~ p.862
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Synthesis of Thienopyrimidine Derivatives as Inhibitors of STAT3
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Jang Hyo-Ju
Kim Sung-Min
Rho Mun-Chual
Lee Seung-Woong
Song Yang-Heon
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Abstract
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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.
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KEYWORD
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Thienopyrimidine derivatives, Interleukin-6, STAT3, anti-inflammatory
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