2-Substituted 1,5-benzothiazepine-based HDAC inhibitors exert anticancer activities on human solid and acute myeloid leukemia cell lines

Simona De Vita,Sara Meninno,Lucia Capasso, Ester Colarusso,Maria Giovanna Chini,Gianluigi Lauro, Romolo Rinaldi, Annalisa De Cicco, Veronica Sian,Stefania Terracciano,Angela Nebbioso,Alessandra Lattanzi,Giuseppe Bifulco

BIOORGANIC & MEDICINAL CHEMISTRY（2023）

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摘要

•Design of a 2-substituted 1,5-benzothiazepine library and its sulphone variants.•Synthesis of enantioenriched forms of benzothiazepine-based compounds.•Evaluation of anticancer properties by cell-free and cell-based assays.•Up-regulation of HDAC inhibition-related key targets.•Sulphone-bearing molecules were more effective than their reduced form.

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关键词

HDAC,Drug design,Molecular docking,Enantioselective synthesis,2-substituted 1,5-benzothiazepine,Anticancer activity

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