Document Report Card

ID: ALA1145944

Journal: J Med Chem

Title: Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors.

Authors: Kim DK, Lee JY, Kim JS, Ryu JH, Choi JY, Lee JW, Im GJ, Kim TK, Seo JW, Park HJ, Yoo J, Park JH, Kim TY, Bang YJ.

Abstract: Inhibitors of histone deacetylases (HDACs) have been shown to induce differentiation and/or apoptosis of human tumor cells. Novel 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides have been prepared as a new class of HDAC inhibitors and evaluated for their antiproliferative activity and HDAC inhibitory activity. Incorporation of a 1,4-phenylene carboxamide linker, shown by 5, and a 4-(dimethylamino)phenyl or 4-(pyrrolidin-1-yl)phenyl group as a cap substructure generated highly potent hydroxamic acid-based HDAC inhibitors 5a and 5b.

CiteXplore: 14667227

DOI: 10.1021/jm030377q