4.5 Article

Discovery of novel N-hydroxy-2-arylisoindoline-4-carboxamides as potent and selective inhibitors of HDAC11

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 28, Issue 12, Pages 2143-2147

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.05.021

Keywords

HDAC11; HDACs; Oncology; Inflammation; Isoindoline; Hydroxamic acid

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N-Hydroxy-2-arylisoindoline-4-carboxamides are potent and selective inhibitors of HDAC11. The discovery, synthesis, and structure activity relationships of this novel series of inhibitors are reported. An advanced analog (FT895) displays promising cellular activity and pharmacokinetic properties that make it a useful tool to study the biology of HDAC11 and its potential use as a therapeutic target for oncology and inflammation indications.

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