• Title/Summary/Keyword: Thienopyrimidine

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

  • Jang, Hyun-Jae;Kim, Sung Min;Rho, Mun-Chual;Lee, Seung Woong;Song, Yang-Heon
    • Journal of Microbiology and Biotechnology
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    • v.29 no.6
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    • pp.856-862
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    • 2019
  • 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.

Microwave-Assisted and Conventional Synthesis of Benzothieno [3,2-e] [1,3,4] triazolo[4,3-c]pyrimidines: A Comparative Study

  • Gaonkar, Santhosh L.;Ahn, Chuljin;Princia, Princia;Shetty, Nitinkumar S.
    • Journal of the Korean Chemical Society
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    • v.58 no.4
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    • pp.388-392
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    • 2014
  • Benzothieno[2,3-d]pyrimidines (2,3,4) and benzothieno[3,2-e][1,3,4]triazolo[4,3-c] pyrimidines (5a-c) were synthesized from the precursor 2-amino-7-oxo-4,5,6,7-tetrahydro-1-benzothiophene-3-carbonitrile 1 by employing the conventional method as well as the microwave irradiation technique. The precursor 2-amino-3-cyanothiophene analogue 1 was synthesized by employing the well-known Gewald reaction. In the present work it has been found that the microwave supported syntheses are more efficient than the conventional classical heating methods. The structures of all the compounds were ascertained by spectral and analytical data.