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@ARTICLE{Reing:856855,
author = {Reßing, Nina and Marquardt, Viktoria and Gertzen,
Christoph and Schöler, Andrea and Schramm, Alexander and
Kurz, Thomas and Gohlke, Holger and Aigner, Achim and Remke,
Marc and Hansen, Finn Kristian},
title = {{D}esign, {S}ynthesis and {B}iological {E}valuation of
β-{P}eptoid-{C}apped {HDAC} {I}nhibitors with
{A}nti-{N}euroblastoma and {A}nti-{G}lioblastoma {A}ctivity},
journal = {MedChemComm},
volume = {10},
number = {7},
issn = {2040-2511},
address = {Cambridge},
publisher = {RSC Publ.},
reportid = {FZJ-2018-06194},
pages = {1109-1115},
year = {2019},
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.},
cin = {JSC / ICS-6 / NIC},
ddc = {540},
cid = {I:(DE-Juel1)JSC-20090406 / I:(DE-Juel1)ICS-6-20110106 /
I:(DE-Juel1)NIC-20090406},
pnm = {511 - Computational Science and Mathematical Methods
(POF3-511) / Forschergruppe Gohlke $(hkf7_20170501)$},
pid = {G:(DE-HGF)POF3-511 / $G:(DE-Juel1)hkf7_20170501$},
typ = {PUB:(DE-HGF)16},
UT = {WOS:000475806000003},
doi = {10.1039/C8MD00454D},
url = {https://juser.fz-juelich.de/record/856855},
}