939435-84-4Relevant academic research and scientific papers
Design and synthesis of a potent histone deacetylase inhibitor
Liu, Tao,Kapustin, Galina,Etzkorn, Felicia A.
, p. 2003 - 2006 (2008/02/01)
Histone deacetylase (HDAC) inhibitors have potential for cancer therapy. An HDAC inhibitor based on a cyclic peptide mimic of known structure, linked by an aliphatic chain to a hydroxamic acid, was designed and synthesized. The chimeric compound showed potent competitive inhibition of nuclear HDACs, with an IC50 value of 46 nM and a Ki value of 13.7 nM. The designed inhibitor showed 4-fold selectivity for HDAC1 (57 nM) over HDAC8 (231 nM).
