Basic Information
ID: ALA3393016
Journal: Bioorg Med Chem Lett
Title: Development of novel Asf1-H3/H4 inhibitors.
Authors: Miknis GF, Stevens SJ, Smith LE, Ostrov DA, Churchill ME.
Abstract: The histone chaperone anti-silencing function 1 (Asf1) has emerged as a promising target for therapeutic intervention for multiple cancers (Cell2006, 127, 458). Asf1 is involved in the packaging of the eukaryotic genome into chromatin, which is essential for normal growth, development, and differentiation, as this regulates all nuclear processes that use DNA as a substrate. Starting from a collection of HTS leads, we identified a series of N-acyl hydrazones as novel inhibitors of the Asf-histone H3/H4 interaction. These compounds represent the first example of inhibitors capable of disrupting the Asf1-H3/H4 complex.
CiteXplore: 25582598
DOI: 10.1016/j.bmcl.2014.11.067
Patent ID: ┄
Associated Items: Associated Bioactivities Associated Assays Associated Compounds Associated Targets