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http://dx.doi.org/10.4014/jmb.1811.11046

Synthesis of Thienopyrimidine Derivatives as Inhibitors of STAT3 Activation Induced by IL-6  

Jang, Hyun-Jae (Immunoregulatory Materials Research Center, Korea Research Institute of Bioscience and Biotechnology)
Kim, Sung Min (Department of Chemistry, Mokwon University)
Rho, Mun-Chual (Immunoregulatory Materials Research Center, Korea Research Institute of Bioscience and Biotechnology)
Lee, Seung Woong (Immunoregulatory Materials Research Center, Korea Research Institute of Bioscience and Biotechnology)
Song, Yang-Heon (Department of Chemistry, Mokwon University)
Publication Information
Journal of Microbiology and Biotechnology / v.29, no.6, 2019 , pp. 856-862 More about this Journal
Abstract
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 $IC_{50}$ values of $5.73-0.32{\mu}M$. 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.
Keywords
Thienopyrimidine derivatives; interleukin-6; STAT3; anti-inflammation;
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