Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors.
Basic Information
ID: ALA4480453
Journal: Bioorg Med Chem
Title: Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors.
Authors: Zhang Q, Lv J, He F, Yu C, Qu Y, Zhang X, Xu A, Wu J.
Abstract: Histone deacetylases inhibitors (HDACIs) represents effective treatments for cancer. In continuing our efforts to develop novel and potent HDACIs, a series of N-hydroxycinnamamide-based HDACIs with aromatic ring and various aliphatic linker have been successfully designed and synthesized. Biological evaluations established that compounds 4h, 4i, 4j, 4l, 4r showed superior inhibition on histone deacetylase and antiproliferative activity in some solid tumor cell lines [HeLa, SK-N-BE(2), PC-3] compared to the known inhibitor SAHA. Among these analogs, 4l exhibited selectivity to HDAC1.
CiteXplore: 30879863
DOI: 10.1016/j.bmc.2019.03.008
Patent ID: ┄