Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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Novel Inhibitors of Prolyl 4-Hydroxylase; Solid-phase Synthesis of 2,2-Dimethyl-3,4-Dialkoxy-Substituted 6-Aminobenzopyran Derivatives

  • Seo, Jin-soo (Medicinal Science Division, Korea Research Institute of Chemical Technology) ;
  • Joo, Yang-Hee (Graduate School of Biotechnology, Korea University) ;
  • Yi, Jung-Bum (SK Chemicals Co. Ltd.) ;
  • Lee, Eun-Ju (SK Chemicals Co. Ltd.) ;
  • Lee, Nam-Kyu (SK Chemicals Co. Ltd.) ;
  • Cho, Yong-Balk (SK Chemicals Co. Ltd.) ;
  • Kwak, Wie-Jong (SK Chemicals Co. Ltd.) ;
  • Hwang, Jong-Yeon (Medicinal Science Division, Korea Research Institute of Chemical Technology) ;
  • Jeon, Yong-Seog (Medicinal Science Division, Korea Research Institute of Chemical Technology) ;
  • Jeon, Hyun-Suk (Medicinal Science Division, Korea Research Institute of Chemical Technology) ;
  • Yoo, Sung-eun (Medicinal Science Division, Korea Research Institute of Chemical Technology) ;
  • Yoon, Cheol-Min (Graduate School of Biotechnology, Korea University) ;
  • Dong, Mi-Sook (Graduate School of Biotechnology, Korea University) ;
  • Gong, Young-Dae (Medicinal Science Division, Korea Research Institute of Chemical Technology)
  • Published : 2006.06.20
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Abstract

2,2-Dimethyl-3,4-dialkoxy-substituted 6-aminobenzopyran analogues (eg., 7 and 8) were identified as prolyl 4-hydroxylase inhibitors via a screening process using HSC-T6 and LI 90 cells that express an immortalized rat hepatic stellate cell line and as part of a test of the type I collagen contents employing the ELISA method. A subsequent lead optimization effort based on solid-phase parallel synthesis led to the identification of 2,2-dimethyl-3,4-dialkoxy-substituted 6-aminobenzopyrans as potent inhibitors of prolyl 4-hydroxylase.

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References

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