Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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Discovery of Novel Transcription Factor Inhibitors Using a Pyrazole-based Small Molecule Library

  • Ha, Hyung-Ho (Department of Chemistry, Seoul National University) ;
  • Kim, B.Moon (Department of Chemistry, Seoul National University)
  • Published : 2008.02.20
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Abstract

A focused library of pyrazole-based compounds was constructed towards novel transcription factor inhibitors. Complementary hydrogen bonding interaction with b-sheet peptide structures was the basis for the design of 5-amino-3-pyrazole carboxamide scaffold. From the preliminary inhibition assay against several transcription factors, compounds 7e and 8g were identified as novel lead compounds against HIF-1a and NF-AT transcription factors, respectively.

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