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http://dx.doi.org/10.5012/bkcs.2008.29.2.323

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)
Publication Information
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.
Keywords
Transcription factor; 5-Amino-3-pyrazole carboxamide; HIF-1α; NF-AT; Inhibitor
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