Discovery of Novel Transcription Factor Inhibitors Using a Pyrazole-based Small Molecule Library

摘要

A focused library of pyrazole-based compounds was constructed towards novel transcription factor inhibitors. Complementary hydrogen bonding interaction with モ-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-1メ and NF-AT transcription factors, respectively.