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| Home > Publications database > Design, Synthesis and Biological Evaluation of β-Peptoid-Capped HDAC Inhibitors with Anti-Neuroblastoma and Anti-Glioblastoma Activity |
| Home > Publications database > Design, Synthesis and Biological Evaluation of β-Peptoid-Capped HDAC Inhibitors with Anti-Neuroblastoma and Anti-Glioblastoma Activity |
| Journal Article | FZJ-2018-06194 |
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2019
RSC Publ.
Cambridge
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Please use a persistent id in citations: doi:10.1039/C8MD00454D
Abstract: Histone deacetylases (HDACs) have been identified as promising epigenetic drug targets for the treatment of neuroblastomaand glioblastoma. In this work, we have rationally designed a novel type of peptoid‐based histone deacetylase inhibitors(HDACi). A mini library of β‐peptoid‐capped HDACi was synthesized using a four‐step protocol. All compounds were screenedin biochemical assays for its inhibition of HDAC1 and HDAC6 and docking studies were performed to rationalize the observedselectivity profile. The synthesized compounds were further examined for tumor cell‐inhibitory activity against a panel ofneuroblastoma and glioblastoma cell lines. In particular, non‐selective compounds with potent activity against HDAC1 andHDAC6 showed strong antiproliferative effects. The most promising HDACi, compound 6i, displayed submicromolar tumorcell‐inhibitory potential (IC50: 0.21 – 0.67 μM) against all five cancer cell lines investigated and exceeded the activity of theFDA‐approved HDACi vorinostat.
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